Nanotechnology-Enabled Strategies to Enhance Topical Bioavailability

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Nanomedicine and Nanotechnology".

Deadline for manuscript submissions: closed (10 June 2022) | Viewed by 31854

Special Issue Editors


E-Mail Website
Guest Editor
Department of Pharmaceutical Technology, Faculty of Pharmacy, “Victor Babes” University of Medicine and Pharmacy, Eftimie Murgu Square, No. 2, 300041 Timisoara, Romania
Interests: topical bioavailability; solid-state preformulation; nanoparticles
Special Issues, Collections and Topics in MDPI journals

E-Mail Website1 Website2
Guest Editor
1. Department of Pharmaceutical Physics, Faculty of Pharmacy, Victor Babeş University of Medicine and Pharmacy Timisoara, 2nd EftimieMurgu Sq., 300041 Timişoara, Romania
2. Research Center for Pharmaco-Toxicological Evaluations, Faculty of Pharmacy, Victor Babes University of Medicine and Pharmacy, 2nd Eftimie Murgu Sq., 300041 Timisoara, Romania
Interests: nanodelivery systems; stimuli-controlled release; bioavailability; in vitro assessments using cell monolayer and 3D human reconstructed microtissues
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The design and development of new topical formulations are trending topics, especially for the biomedical field, as they can be conceived to not only address protective and cosmetic needs, but also target therapeutic outcomes.

Because one of the main functions of human skin is protection—the skin acting as a barrier to the penetration of various external factors—the penetration of active substances through the skin is impaired, thus limiting their therapeutic potential. To overcome this, innovative strategies are required to increase skin permeability by means of penetration promoters.

In this regard, modern nanotechnology-based formulations are being developed, such as derived liposomal formulations (transferosomes, ethosomes, cubosomes, nanostructured lipid carriers or other lipid-based nanocarriers), nanogels, nanoemulsions, cyclodextrin-based formulations and other modern approaches.

For the current Special Issue, original research and review articles addressing recent advances in nanopharmaceutical formulations with enhanced topical bioavailability and complex biological in vitro and/or in vivo profiles are welcomed.

Dr. Lenuţa Maria Şuta
Dr. Claudia Geanina Watz
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceutics is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • nanotechnology-based formulations
  • drug-in nanocarriers
  • cyclodextrin-in nanocarriers
  • polymer-based nanocarriers
  • topical drug-delivery systems
  • bioavailability enhancement
  • drug release
  • in vitro and in vivo skin models
  • biological assessment

Related Special Issue

Published Papers (12 papers)

Order results
Result details
Select all
Export citation of selected articles as:

Research

Jump to: Review

14 pages, 3422 KiB  
Article
Encapsulation of Human-Bone-Marrow-Derived Mesenchymal Stem Cells in Small Alginate Beads Using One-Step Emulsification by Internal Gelation: In Vitro, and In Vivo Evaluation in Degenerate Intervertebral Disc Model
by Sarit S. Sivan, Iris Bonstein, Yariv N. Marmor, Gadi Pelled, Zulma Gazit and Michal Amit
Pharmaceutics 2022, 14(6), 1179; https://doi.org/10.3390/pharmaceutics14061179 - 31 May 2022
Cited by 6 | Viewed by 2079
Abstract
Cell microencapsulation in gel beads contributes to many biomedical processes and pharmaceutical applications. Small beads (<300 µm) offer distinct advantages, mainly due to improved mass transfer and mechanical strength. Here, we describe, for the first time, the encapsulation of human-bone-marrow-derived mesenchymal stem cells [...] Read more.
Cell microencapsulation in gel beads contributes to many biomedical processes and pharmaceutical applications. Small beads (<300 µm) offer distinct advantages, mainly due to improved mass transfer and mechanical strength. Here, we describe, for the first time, the encapsulation of human-bone-marrow-derived mesenchymal stem cells (hBM-MSCs) in small-sized microspheres, using one-step emulsification by internal gelation. Small (127–257 µm) high-mannuronic-alginate microspheres were prepared at high agitation rates (800–1000 rpm), enabling control over the bead size and shape. The average viability of encapsulated hBM-MSCs after 2 weeks was 81 ± 4.3% for the higher agitation rates. hBM-MSC-loaded microspheres seeded within a glycosaminoglycan (GAG) analogue, which was previously proposed as a mechanically equivalent implant for degenerate discs, kept their viability, sphericity, and integrity for at least 6 weeks. A preliminary in vivo study of hBM-MSC-loaded microspheres implanted (via a GAG-analogue hydrogel) in a rat injured intervertebral disc model demonstrated long-lasting viability and biocompatibility for at least 8 weeks post-implantation. The proposed method offers an effective and reproducible way to maintain long-lasting viability in vitro and in vivo. This approach not only utilizes the benefits of a simple, mild, and scalable method, but also allows for the easy control of the bead size and shape by the agitation rate, which, overall, makes it a very attractive platform for regenerative-medicine applications. Full article
(This article belongs to the Special Issue Nanotechnology-Enabled Strategies to Enhance Topical Bioavailability)
Show Figures

Figure 1

20 pages, 3874 KiB  
Article
Ethosomes and Transethosomes as Cutaneous Delivery Systems for Quercetin: A Preliminary Study on Melanoma Cells
by Francesca Ferrara, Mascia Benedusi, Maddalena Sguizzato, Rita Cortesi, Anna Baldisserotto, Raissa Buzzi, Giuseppe Valacchi and Elisabetta Esposito
Pharmaceutics 2022, 14(5), 1038; https://doi.org/10.3390/pharmaceutics14051038 - 11 May 2022
Cited by 23 | Viewed by 3116
Abstract
The present study is aimed to design ethosomes and transethosomes for topical administration of quercetin. To overcome quercetin low bioavailability, scarce solubility and poor permeability that hamper its pharmaceutical use, the drug was loaded in ethosomes and transethosomes based on different concentrations of [...] Read more.
The present study is aimed to design ethosomes and transethosomes for topical administration of quercetin. To overcome quercetin low bioavailability, scarce solubility and poor permeability that hamper its pharmaceutical use, the drug was loaded in ethosomes and transethosomes based on different concentrations of phosphatidylcholine. Vesicle morphology was studied by cryogenic transmission electron microscopy, while size distribution and quercetin entrapment capacity were evaluated up to 3 months, respectively, by photon correlation spectroscopy and high-performance liquid chromatography. The antioxidant property was studied by photochemiluminescence test. Quercetin release and permeation was investigated in vitro, using Franz cells associated to different membranes. In vitro assays were conducted on human keratinocytes and melanoma cells to study the behavior of quercetin-loaded nano-vesicular forms with respect to cell migration and proliferation. The results evidenced that both phosphatidylcholine concentration and quercetin affected the vesicle size. Quercetin entrapment capacity, antioxidant activity and size stability were controlled using transethosomes produced by the highest amount of phosphatidylcholine. In vitro permeation studies revealed an enhancement of quercetin permeation in the case of transethosomes with respect to ethosomes. Notably, scratch wound and migration assays suggested the potential of quercetin loaded-transethosomes as adjuvant strategy for skin conditions. Full article
(This article belongs to the Special Issue Nanotechnology-Enabled Strategies to Enhance Topical Bioavailability)
Show Figures

Graphical abstract

12 pages, 1880 KiB  
Article
Potential UV-Protective Effect of Freestanding Biodegradable Nanosheet-Based Sunscreen Preparations in XPA-Deficient Mice
by Tomomi Hatanaka, Khampeeraphan Ramphai, Shun Takimoto, Hiromi Kanda, Nami Motosugi, Minoru Kimura, Tomotaka Mabuchi, Midori Oyama, Tomoharu Takeuchi and Yosuke Okamura
Pharmaceutics 2022, 14(2), 431; https://doi.org/10.3390/pharmaceutics14020431 - 17 Feb 2022
Viewed by 1896
Abstract
Xeroderma pigmentosum (XP) is a rare autosomal recessive hereditary disorder. As patients with XP are deficient in nucleotide excision repair, they show severe photosensitivity symptoms. Although skin protection from ultraviolet (UV) radiation is essential to improve the life expectancy of such patients, the [...] Read more.
Xeroderma pigmentosum (XP) is a rare autosomal recessive hereditary disorder. As patients with XP are deficient in nucleotide excision repair, they show severe photosensitivity symptoms. Although skin protection from ultraviolet (UV) radiation is essential to improve the life expectancy of such patients, the optimal protective effect is not achieved even with sunscreen application, owing to the low usability of the preparations. Nanosheets are two-dimensional nanostructures with a thickness in the nanometer range. The extremely large aspect ratios of the nanosheets result in high transparency, flexibility, and adhesiveness. Moreover, their high moisture permeability enables their application to any area of the skin for a long time. We fabricated preparations containing avobenzone (BMDBM) based on freestanding poly (L-lactic acid) (PLLA) nanosheets through a spin-coating process. Although monolayered PLLA nanosheets did not contain enough BMDBM to protect against UV radiation, the layered nanosheets, consisting of five discrete BMDBM nanosheets, showed high UV absorbance without lowering the adhesive strength against skin. Inflammatory reactions in XPA-deficient mice after UV radiation were completely suppressed by the application of BMDBM-layered nanosheets to the skin. Thus, the BMDBM layered nanosheet could serve as a potential sunscreen preparation to improve the quality of life of patients with XP. Full article
(This article belongs to the Special Issue Nanotechnology-Enabled Strategies to Enhance Topical Bioavailability)
Show Figures

Graphical abstract

23 pages, 3555 KiB  
Article
An Update to Dialysis-Based Drug Release Testing—Data Analysis and Validation Using the Pharma Test Dispersion Releaser
by Marc-Phillip Mast, Harshvardhan Modh, Julian Knoll, Elena Fecioru and Matthias G. Wacker
Pharmaceutics 2021, 13(12), 2007; https://doi.org/10.3390/pharmaceutics13122007 - 25 Nov 2021
Cited by 8 | Viewed by 3195
Abstract
Currently, a wide variety of complex non-oral dosage forms are entering the global healthcare market. Although many assays have been described in recent research, harmonized procedures and standards for testing their in vitro performance remain widely unexplored. Among others, dialysis-based techniques such as [...] Read more.
Currently, a wide variety of complex non-oral dosage forms are entering the global healthcare market. Although many assays have been described in recent research, harmonized procedures and standards for testing their in vitro performance remain widely unexplored. Among others, dialysis-based techniques such as the Pharma Test Dispersion Releaser are developed for testing the release of drugs from nanoparticles, liposomes, or extracellular vesicle preparations. Here, we provide advanced strategies and practical advice for the development and validation of dialysis-based techniques, including documentation, analysis, and interpretation of the raw data. For this purpose, key parameters of the release assay, including the hydrodynamics in the device at different stirring rates, the selectivity for particles and molecules, as well as the effect of excipients on drug permeation were investigated. At the highest stirring rate, a more than twofold increase in the membrane permeation rate (from 0.99 × 10−3 to 2.17 × 10−3 cm2/h) was observed. Additionally, we designed a novel computer model to identify important quality parameters of the dialysis experiment and to calculate error-corrected release profiles. Two hydrophilic creams of diclofenac, Voltaren® Emulgel, and Olfen® gel, were tested and provide first-hand evidence of the robustness of the assay in the presence of semisolid dosage forms. Full article
(This article belongs to the Special Issue Nanotechnology-Enabled Strategies to Enhance Topical Bioavailability)
Show Figures

Graphical abstract

15 pages, 29945 KiB  
Article
Instillation of Ophthalmic Formulation Containing Nilvadipine Nanocrystals Attenuates Lens Opacification in Shumiya Cataract Rats
by Ryoka Goto, Shigehiro Yamada, Hiroko Otake, Yosuke Nakazawa, Mikako Oka, Naoki Yamamoto, Hiroshi Sasaki and Noriaki Nagai
Pharmaceutics 2021, 13(12), 1999; https://doi.org/10.3390/pharmaceutics13121999 - 25 Nov 2021
Cited by 2 | Viewed by 1694
Abstract
We developed ophthalmic formulations based on nilvadipine (NIL) nanocrystals (NIL-NP dispersions; mean particle size: 98 nm) by using bead mill treatment and investigated whether the instillation of NIL-NP dispersions delivers NIL to the lens and prevents lens opacification in hereditary cataractous Shumiya cataract [...] Read more.
We developed ophthalmic formulations based on nilvadipine (NIL) nanocrystals (NIL-NP dispersions; mean particle size: 98 nm) by using bead mill treatment and investigated whether the instillation of NIL-NP dispersions delivers NIL to the lens and prevents lens opacification in hereditary cataractous Shumiya cataract rats (SCRs). Serious corneal stimulation was not detected in either human corneal epithelial cells or rats treated with NIL-NP dispersions. The NIL was directly delivered to the lens by the instillation of NIL-NP dispersions, and NIL content in the lenses of rats instilled with NIL-NP dispersions was significantly higher than that in the ophthalmic formulations based on NIL microcrystals (NIL-MP dispersions; mean particle size: 21 µm). Moreover, the supply of NIL prevented increases in Ca2+ content and calpain activity in the lenses of SCRs and delayed the onset of cataracts. In addition, the anti-cataract effect in the lens of rats instilled with NIL-NP dispersions was also significantly higher than that in NIL-MP dispersions. NIL-NPs could be used to prevent lens opacification. Full article
(This article belongs to the Special Issue Nanotechnology-Enabled Strategies to Enhance Topical Bioavailability)
Show Figures

Graphical abstract

20 pages, 11715 KiB  
Article
Green Synthesized Silver Nanoparticles Using Tridax Procumbens for Topical Application: Excision Wound Model and Histopathological Studies
by Farhat Fatima, Mohammed F. Aldawsari, Mohammed Muqtader Ahmed, Md. Khalid Anwer, Maimuna Naz, Mohammad Javed Ansari, Abubaker M. Hamad, Ameeduzzafar Zafar and Mohammed Jafar
Pharmaceutics 2021, 13(11), 1754; https://doi.org/10.3390/pharmaceutics13111754 - 21 Oct 2021
Cited by 21 | Viewed by 3734
Abstract
The objective of this study was to synthesize silver nanoparticles from the leaves of Tridax procumbens and develop its topical gels using chitosan to investigate the wound healing efficacy concomitant with the histopathological study. Green synthesized silver nanoparticles (AgNPs) were prepared by reacting [...] Read more.
The objective of this study was to synthesize silver nanoparticles from the leaves of Tridax procumbens and develop its topical gels using chitosan to investigate the wound healing efficacy concomitant with the histopathological study. Green synthesized silver nanoparticles (AgNPs) were prepared by reacting silver nitrate (0.3 M) with leaf extract and characterized by particle analysis, FTIR, XRD, SEM, BET, and TGA. The results revealed formed AgNPs were nano-sized (138 ± 2.1 nm), monodispersed (PDI: 0.460 ± 0.3), inter-particle repulsion (zeta: −20.4 ± 5.20 mV), stabilized, crystalline and, spherical with size ranging from 80–100 nm as per SEM micro photos. The BET analysis of AgNPs presents the surface area (12.861 m2/g), pore volume (0.037 cc/g), and pore radius (24.50 nm).TGA results show a loss of 13.39% up to 300 °C. The topical formulation was developed by loading AgNPs in chitosan-based gels, evaluated by pH, thermal cycling, centrifugal, and spreadability tests. AgNPs chitosan gels results showed skin compatibility, higher stability, and spreading ability. The maximum antibacterial zone of inhibition was found to be 25 ± 0.98 mm for bacillus subtitles and 30 ± 1.99 mm for Klebsiella pneumoniae, respectively. Nanosilver-containing gel also showed excellent compatibility with erythrocytes. Excision wound model was used to assess the wound healing property of the developed AgNP gels, the results of which indicated a significantly progressive healing process in test-group of animals treated with chitosan-based gels containing AgNPs. A histopathological study further confirmed the almost normal skin structure of treated animal tissue compared to standard and negative control. Thus, green synthesized AgNPs loaded chitosan-based topical gel can potentially be used for wound healing application. Full article
(This article belongs to the Special Issue Nanotechnology-Enabled Strategies to Enhance Topical Bioavailability)
Show Figures

Graphical abstract

21 pages, 6032 KiB  
Article
Antimicrobial Activities of Chitosan Derivatives
by Cristina Ardean, Corneliu Mircea Davidescu, Nicoleta Sorina Nemeş, Adina Negrea, Mihaela Ciopec, Narcis Duteanu, Petru Negrea, Daniel Duda-Seiman and Delia Muntean
Pharmaceutics 2021, 13(10), 1639; https://doi.org/10.3390/pharmaceutics13101639 - 08 Oct 2021
Cited by 12 | Viewed by 1823
Abstract
Considering the challenge created by the development of bacterial and fungal strains resistant to multiple therapeutic variants, new molecules and materials with specific properties against these microorganisms can be synthesized, like those synthesized from biopolymers such as chitosan with improved antimicrobial activities. Antimicrobial [...] Read more.
Considering the challenge created by the development of bacterial and fungal strains resistant to multiple therapeutic variants, new molecules and materials with specific properties against these microorganisms can be synthesized, like those synthesized from biopolymers such as chitosan with improved antimicrobial activities. Antimicrobial activities of seven obtained materials were tested on four reference strains belonging to American Type Culture Collection. The best antimicrobial activity was obtained by functionalization by impregnation of chitosan with quaternary ammonium salts, followed by that obtained by functionalization of chitosan with phosphonium. The lowest antibacterial and antifungal effects were expressed by Ch-THIO and Ch-MBT, but new materials obtained with these extractants may be precursors with a significant role in the direct control of active molecules, such as cell growth factors or cell signaling molecules. Full article
(This article belongs to the Special Issue Nanotechnology-Enabled Strategies to Enhance Topical Bioavailability)
Show Figures

Figure 1

24 pages, 3046 KiB  
Article
Comparative Study of the Pharmacological Properties and Biological Effects of Polygonum aviculare L. herba Extract-Entrapped Liposomes versus Quercetin-Entrapped Liposomes on Doxorubicin-Induced Toxicity on HUVECs
by Mariana Mureşan, Diana Olteanu, Gabriela Adriana Filip, Simona Clichici, Ioana Baldea, Tunde Jurca, Annamaria Pallag, Eleonora Marian, Adina Frum, Felicia Gabriela Gligor, Paula Svera, Bogdan Stancu and Laura Vicaș
Pharmaceutics 2021, 13(9), 1418; https://doi.org/10.3390/pharmaceutics13091418 - 07 Sep 2021
Cited by 15 | Viewed by 2974
Abstract
This study aimed to evaluate the comparative biological effects of Polygonum aviculare L. herba (PAH) extract and quercetin-entrapped liposomes on doxorubicin (Doxo)-induced toxicity in HUVECs. HUVECs were treated with two formulations of liposomes loaded with PAH extract (L5 and L6) and two formulations [...] Read more.
This study aimed to evaluate the comparative biological effects of Polygonum aviculare L. herba (PAH) extract and quercetin-entrapped liposomes on doxorubicin (Doxo)-induced toxicity in HUVECs. HUVECs were treated with two formulations of liposomes loaded with PAH extract (L5 and L6) and two formulations of liposomes loaded with quercetin (L3 prepared with phosphatidylcholine and L4 prepared with phosphatidylserine). The results obtained with atomic force microscopy, zeta potential and entrapment liposome efficiency confirmed the interactions of the liposomes with PAH or free quercetin and a controlled release of flavonoids entrapped in all the liposomes. Doxo decreased the cell viability and induced oxidative stress, inflammation, DNA lesions and apoptosis in parallel with the activation of Nrf2 and NF-kB. Free quercetin, L3 and L4 inhibited the oxidative stress and inflammation and reduced apoptosis, particularly L3. Additionally, these compounds diminished the Nrf2 and NF-kB expressions and DNA lesions, principally L4. PAH extract, L5 and L6 exerted antioxidant and anti-inflammatory activities, reduced γH2AX formation and inhibited extrinsic apoptosis and transcription factors activation but to a lesser extent. The loading of quercetin in liposomes increased the cell viability and exerted better endothelial protection compared to free quercetin, especially L3. The liposomes with PAH extract had moderate efficiency, mainly due to the antioxidant and anti-inflammatory effects and the inhibition of extrinsic apoptosis. Full article
(This article belongs to the Special Issue Nanotechnology-Enabled Strategies to Enhance Topical Bioavailability)
Show Figures

Figure 1

15 pages, 4084 KiB  
Article
Nanostructured Lipid Carrier Gel Formulation of Recombinant Human Thrombomodulin Improve Diabetic Wound Healing by Topical Administration
by Yuan-Shuo Hsueh, Yan-Jye Shyong, Hsiu-Ching Yu, Shu-Jhen Jheng, Shang-Wen Lin, Hua-Lin Wu and Jui-Chen Tsai
Pharmaceutics 2021, 13(9), 1386; https://doi.org/10.3390/pharmaceutics13091386 - 02 Sep 2021
Cited by 11 | Viewed by 2771
Abstract
Recombinant human thrombomodulin (rhTM), an angiogenesis factor, has been demonstrated to stimulate cell proliferation, keratinocyte migration and wound healing. The objective of this study was to develop nanostructured lipid carrier (NLC) formulations encapsulating rhTM for promoting chronic wound healing. RhTM-loaded NLCs were prepared [...] Read more.
Recombinant human thrombomodulin (rhTM), an angiogenesis factor, has been demonstrated to stimulate cell proliferation, keratinocyte migration and wound healing. The objective of this study was to develop nanostructured lipid carrier (NLC) formulations encapsulating rhTM for promoting chronic wound healing. RhTM-loaded NLCs were prepared and characterized. Encapsulation efficiency was more than 92%. The rate of rhTM release from different NLC formulations was influenced by their lipid compositions and was sustained for more than 72 h. Studies on diabetic mouse wound model suggested that rhTM-NLC 1.2 µg accelerated wound healing and was similar to recombinant human epidermal growth factor-NLC (rhEGF-NLC) 20 µg. By incorporating 0.085% carbopol (a highly crosslinked polyacrylic acid polymer) into rhTM NLC, the NLC-gel presented similar particle characteristics, and demonstrated physical stability, sustained release property and stability within 12 weeks. Both rhTM NLC and rhTM NLC-gel improved wound healing of diabetic mice and cell migration of human epidermal keratinocyte cell line (HaCaT) significantly. In comparison with rhTM solution, plasma concentrations of rhTM post applications of NLC and NLC-gel formulations were lower and more sustained in 24 h. The developed rhTM NLC and rhTM NLC-gel formulations are easy to prepare, stable and convenient to apply to the wound with reduced systemic exposure, which may warrant potential delivery systems for the care of chronic wound patients. Full article
(This article belongs to the Special Issue Nanotechnology-Enabled Strategies to Enhance Topical Bioavailability)
Show Figures

Figure 1

16 pages, 3184 KiB  
Article
Topical Artocarpus communis Nanoparticles Improved the Water Solubility and Skin Permeation of Raw A. communis Extract, Improving Its Photoprotective Effect
by Chun-Yin Yang, Pao-Hsien Huang, Chih-Hua Tseng and Feng-Lin Yen
Pharmaceutics 2021, 13(9), 1372; https://doi.org/10.3390/pharmaceutics13091372 - 31 Aug 2021
Cited by 4 | Viewed by 1817
Abstract
Antioxidants from plant extracts are often used as additives in skincare products to prevent skin problems induced by environmental pollutants. Artocarpus communis methanol extract (ACM) has many biological effects, such as antioxidant, anti-inflammatory, wound healing, and photoprotective effects; however, the poor water solubility [...] Read more.
Antioxidants from plant extracts are often used as additives in skincare products to prevent skin problems induced by environmental pollutants. Artocarpus communis methanol extract (ACM) has many biological effects, such as antioxidant, anti-inflammatory, wound healing, and photoprotective effects; however, the poor water solubility of raw ACM has limited its applications in medicine and cosmetics. Topical antioxidant nanoparticles are one of the drug-delivery systems for overcoming the poor water solubility of antioxidants for increasing their skin penetration. The present study demonstrated that ACM-loaded hydroxypropyl-β-cyclodextrin and polyvinylpyrrolidone K30 nanoparticles (AHP) were successfully prepared and could effectively increase the skin penetration of ACM through changing the physicochemical characteristics of raw ACM, including reducing the particle size, increasing the surface area, and inducing amorphous transformation. Our results also revealed that AHP had significantly better antioxidant activity than raw ACM for preventing photocytotoxicity because the AHP formulation increased the cellular uptake of the ACM in UVB-irradiated HaCaT keratinocytes. In conclusion, our results suggest that AHP may be used as a good topical antioxidant nanoparticle for delivering ACM into deep layers of the skin for preventing UVB-induced skin problems. Full article
(This article belongs to the Special Issue Nanotechnology-Enabled Strategies to Enhance Topical Bioavailability)
Show Figures

Figure 1

12 pages, 2236 KiB  
Article
Investigating the Potential of Transdermal Delivery of Avanafil Using Vitamin E-TPGS Based Mixed Micelles Loaded Films
by Abdullah A. Alamoudi, Osama A. A. Ahmed and Khalid M. El-Say
Pharmaceutics 2021, 13(5), 739; https://doi.org/10.3390/pharmaceutics13050739 - 17 May 2021
Cited by 5 | Viewed by 2204
Abstract
To avoid the first-pass metabolism of avanafil (AVA) and its altered absorption in the presence of food after oral administration, this study aimed to investigate the potential of TPGS-based mixed micelle (MM)-loaded film for transdermal delivery and the enhancement of bioavailability. A Box–Behnken [...] Read more.
To avoid the first-pass metabolism of avanafil (AVA) and its altered absorption in the presence of food after oral administration, this study aimed to investigate the potential of TPGS-based mixed micelle (MM)-loaded film for transdermal delivery and the enhancement of bioavailability. A Box–Behnken design was employed to optimize the permeation behavior of AVA from the transdermal film across the skin. The variables were the hydrophile-lipophile balance (HLB) of the surfactant (X1), the concentration of mixed micelles (MMs) in the film (X2), and the concentration of the permeation enhancer (X3). The initial permeation of AVA after 1 h (Y1), and the cumulative permeation of AVA after 24 h (Y2) were the dependent variables. Ex vivo studies were carried out on freshly isolated rat skin to investigate the drug’s permeation potential and results were visualized using a fluorescence laser microscope. Moreover, the pharmacokinetic behavior after a single application on male Wistar rats, in comparison with films loaded with raw AVA, was evaluated. The results showed that the optimum factor levels were 9.4% for the HLB of the surfactant used, and 5.12% MMs and 2.99% penetration enhancer in the film. Imaging with a fluorescence laser microscope indicated the ability of the optimized film to deliver the payload to deeper skin layers. Furthermore, optimized AVA-loaded TPGS-micelles film showed a significant increase (p < 0.05) in the Cmax of AVA and the area under the AVA plasma curve (approximately three-fold). The optimized AVA-loaded TPGS-MM film thus represents a successful delivery system for enhancing the bioavailability of AVA. Full article
(This article belongs to the Special Issue Nanotechnology-Enabled Strategies to Enhance Topical Bioavailability)
Show Figures

Graphical abstract

Review

Jump to: Research

38 pages, 1737 KiB  
Review
Vesicular Nanocarriers for Phytocompounds in Wound Care: Preparation and Characterization
by Diana Antonia Safta, Cătălina Bogdan and Mirela Liliana Moldovan
Pharmaceutics 2022, 14(5), 991; https://doi.org/10.3390/pharmaceutics14050991 - 05 May 2022
Cited by 10 | Viewed by 2919
Abstract
The need to develop wound healing preparations is a pressing challenge given the limitations of the current treatment and the rising prevalence of impaired healing wounds. Although herbal extracts have been used for many years to treat skin disorders, due to their wound [...] Read more.
The need to develop wound healing preparations is a pressing challenge given the limitations of the current treatment and the rising prevalence of impaired healing wounds. Although herbal extracts have been used for many years to treat skin disorders, due to their wound healing, anti-inflammatory, antimicrobial, and antioxidant effects, their efficacy can be questionable because of their poor bioavailability and stability issues. Nanotechnology offers an opportunity to revolutionize wound healing therapies by including herbal compounds in nanosystems. Particularly, vesicular nanosystems exhibit beneficial properties, such as biocompatibility, targeted and sustained delivery capacity, and increased phytocompounds’ bioavailability and protection, conferring them a great potential for future applications in wound care. This review summarizes the beneficial effects of phytocompounds in wound healing and emphasizes the advantages of their entrapment in vesicular nanosystems. Different types of lipid nanocarriers are presented (liposomes, niosomes, transferosomes, ethosomes, cubosomes, and their derivates’ systems), highlighting their applications as carriers for phytocompounds in wound care, with the presentation of the state-of-art in this field. The methods of preparation, characterization, and evaluation are also described, underlining the properties that ensure good in vitro and in vivo performance. Finally, future directions of topical systems in which vesicle-bearing herbal extracts or phytocompounds can be incorporated are pointed out, as their development is emerging as a promising strategy. Full article
(This article belongs to the Special Issue Nanotechnology-Enabled Strategies to Enhance Topical Bioavailability)
Show Figures

Figure 1

Back to TopTop