Editorial

7 pages, 352 KiB

Open AccessEditorial

Polymers Enhancing Bioavailability in Drug Delivery

by Ana I. Fernandes and Angela F. Jozala

Pharmaceutics 2022, 14(10), 2199; https://doi.org/10.3390/pharmaceutics14102199 - 16 Oct 2022

Cited by 5 | Viewed by 1590

A drug’s bioavailability, i.e., the extent to and rate at which it enters the systemic circulation, thus accessing the site of action, is largely determined by the properties of the drug [...] Full article

(This article belongs to the Special Issue Polymers Enhancing Bioavailability in Drug Delivery)

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Research

Jump to: Editorial, Review

21 pages, 7708 KiB

Open AccessArticle

Enhancement of the Bioavailability and Anti-Inflammatory Activity of Glycyrrhetinic Acid via Novel Soluplus^®—A Glycyrrhetinic Acid Solid Dispersion

by Hao Wang, Runwei Li, Yuan Rao, Saixing Liu, Chunhui Hu, Yong Zhang, Linchao Meng, Qilin Wu, Qiuhong Ouyang, Hao Liang and Meng Qin

Pharmaceutics 2022, 14(9), 1797; https://doi.org/10.3390/pharmaceutics14091797 - 26 Aug 2022

Cited by 9 | Viewed by 2182

Abstract

Glycyrrhetinic acid (GA) is an anti-inflammatory drug with potential for development. However, the poor solubility of GA in water leads to extremely low bioavailability, which limits its clinical applications. Solid dispersions have become some of the most effective strategies for improving the solubility [...] Read more.

Glycyrrhetinic acid (GA) is an anti-inflammatory drug with potential for development. However, the poor solubility of GA in water leads to extremely low bioavailability, which limits its clinical applications. Solid dispersions have become some of the most effective strategies for improving the solubility of poorly soluble drugs. Soluplus^®, a non-cytotoxic amphiphilic solubilizer, significantly improves the solubility of BCS II drugs and improves the bioavailability of insoluble drugs. l-arginine (L-Arg) can be used as a small molecular weight excipient to assist in improving the solubility of insoluble drugs. In this study, we developed a new formulation for oral administration by reacting GA and L-Arg to form salts by co-solvent evaporation and then adding the polymer-solvent Soluplus^® with an amphiphilic chemical structure to prepare a solid dispersion GA-SD. The chemical and physical properties of GA-SD were characterized by DLS, TEM, XRD, FT-IR and TG. The anti-inflammatory activity of GA-SD was verified by LPS stimulation of RAW 267.5 cells simulating a cellular inflammation model, TPA-induced ear edema model in mice, and ethanol-induced gastric ulcer model. The results showed that the amide bond and salt formation of GA-SD greatly improved GA solubility. GA-SD effectively improved the anti-inflammatory effect of free GA in vivo and in vitro, and GA-SD had no significant effect on liver and kidney function, no significant tissue toxicity, and good biosafety. In conclusion, GA-SD with L-Arg and Soluplus^® is an effective method to improve the solubility and bioavailability of GA. As a safe and effective solid dispersion, it is a promising anti-inflammatory oral formulation and provides some references for other oral drug candidates with low bioavailability. Full article

(This article belongs to the Special Issue Polymers Enhancing Bioavailability in Drug Delivery)

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15 pages, 10118 KiB

Open AccessArticle

Leveraging Affinity Interactions to Prolong Drug Delivery of Protein Therapeutics

by Alan B. Dogan, Katherine E. Dabkowski and Horst A. von Recum

Pharmaceutics 2022, 14(5), 1088; https://doi.org/10.3390/pharmaceutics14051088 - 19 May 2022

Cited by 6 | Viewed by 1900

Abstract

While peptide and protein therapeutics have made tremendous advances in clinical treatments over the past few decades, they have been largely hindered by their ability to be effectively delivered to patients. While bolus parenteral injections have become standard clinical practice, they are insufficient [...] Read more.

While peptide and protein therapeutics have made tremendous advances in clinical treatments over the past few decades, they have been largely hindered by their ability to be effectively delivered to patients. While bolus parenteral injections have become standard clinical practice, they are insufficient to treat diseases that require sustained, local release of therapeutics. Cyclodextrin-based polymers (pCD) have been utilized as a platform to extend the local delivery of small-molecule hydrophobic drugs by leveraging hydrophobic-driven thermodynamic interactions between pCD and payload to extend its release, which has seen success both in vitro and in vivo. Herein, we proposed the novel synthesis of protein–polymer conjugates that are capped with a “high affinity” adamantane. Using bovine serum albumin as a model protein, and anti-interleukin 10 monoclonal antibodies as a functional example, we outline the synthesis of novel protein–polymer conjugates that, when coupled with cyclodextrin delivery platforms, can maintain a sustained release of up to 65 days without largely sacrificing protein structure/function which has significant clinical applications in local antibody-based treatments for immune diseases, cancers, and diabetes. Full article

(This article belongs to the Special Issue Polymers Enhancing Bioavailability in Drug Delivery)

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13 pages, 2341 KiB

Open AccessArticle

Formulation and Characterization of Stimuli-Responsive Lecithin-Based Liposome Complexes with Poly(acrylic acid)/Poly(N,N-dimethylaminoethyl methacrylate) and Pluronic^® Copolymers for Controlled Drug Delivery

by Mónica G. Simões, Ayelen Hugo, Andrea Gómez-Zavaglia, Pedro N. Simões and Patrícia Alves

Pharmaceutics 2022, 14(4), 735; https://doi.org/10.3390/pharmaceutics14040735 - 29 Mar 2022

Cited by 3 | Viewed by 2420

Abstract

Polymer–liposome complexes (PLCs) can be efficiently applied for the treatment and/or diagnosis of several types of diseases, such as cancerous, dermatological, neurological, ophthalmic and orthopedic. In this work, temperature-/pH-sensitive PLC-based systems for controlled release were developed and characterized. The selected hydrophilic polymeric setup [...] Read more.

Polymer–liposome complexes (PLCs) can be efficiently applied for the treatment and/or diagnosis of several types of diseases, such as cancerous, dermatological, neurological, ophthalmic and orthopedic. In this work, temperature-/pH-sensitive PLC-based systems for controlled release were developed and characterized. The selected hydrophilic polymeric setup consists of copolymers of Pluronic^®-poly(acrylic acid) (PLU-PAA) and Pluronic^®-poly(N,N-dimethylaminoethyl methacrylate) (PLU-PD) synthesized by atom transfer radical polymerization (ATRP). The copolymers were incorporated into liposomes formulated from soybean lecithin, with different copolymer/phospholipid ratios (2.5, 5 and 10%). PLCs were characterized by evaluating their particle size, polydispersity, surface charge, capacity of release and encapsulation efficiency. Their cytotoxic potential was assessed by determining the viability of human epithelial cells exposed to them. The results showed that the incorporation of the synthesized copolymers positively contributed to the stabilization of the liposomes. The main accomplishments of this work were the innovative synthesis of PLU-PD and PLU-PAA by ATRP, and the liposome stabilization by their incorporation. The formulated PLCs exhibited relevant characteristics, notably stimuli-responsive attributes upon slight changes in pH and/or temperature, with proven absence of cellular toxicity, which could be of interest for the treatment or diagnosis of all diseases that cause some particular pH/temperature change in the target area. Full article

(This article belongs to the Special Issue Polymers Enhancing Bioavailability in Drug Delivery)

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16 pages, 1791 KiB

Open AccessArticle

Oromucosal Alginate Films with Zein Nanoparticles as a Novel Delivery System for Digoxin

by Daniela A. Rodrigues, Sónia P. Miguel, Jorge Loureiro, Maximiano Ribeiro, Fátima Roque and Paula Coutinho

Pharmaceutics 2021, 13(12), 2030; https://doi.org/10.3390/pharmaceutics13122030 - 29 Nov 2021

Cited by 7 | Viewed by 2862

Abstract

Digoxin is a hydrophobic drug used for the treatment of heart failure that possesses a narrow therapeutic index, which raises safety concerns for toxicity. This is of utmost relevance in specific populations, such as the elderly. This study aimed to demonstrate the potential [...] Read more.

Digoxin is a hydrophobic drug used for the treatment of heart failure that possesses a narrow therapeutic index, which raises safety concerns for toxicity. This is of utmost relevance in specific populations, such as the elderly. This study aimed to demonstrate the potential of the sodium alginate films as buccal drug delivery system containing zein nanoparticles incorporated with digoxin to reduce the number of doses, facilitating the administration with a quick onset of action. The film was prepared using the solvent casting method, whereas nanoparticles by the nanoprecipitation method. The nanoparticles incorporated with digoxin (0.25 mg/mL) exhibited a mean size of 87.20 ± 0.88 nm, a polydispersity index of 0.23 ± 0.00, and a zeta potential of 21.23 ± 0.07 mV. Digoxin was successfully encapsulated into zein nanoparticles with an encapsulation efficiency of 91% (±0.00). Films with/without glycerol and with different concentrations of ethanol were produced. The sodium alginate (SA) films with 10% ethanol demonstrated good performance for swelling (maximum of 1474%) and mechanical properties, with a mean tensile strength of 0.40 ± 0.04 MPa and an elongation at break of 27.85% (±0.58), compatible with drug delivery application into the buccal mucosa. The current study suggests that SA films with digoxin-loaded zein nanoparticles can be an effective alternative to the dosage forms available on the market for digoxin administration. Full article

(This article belongs to the Special Issue Polymers Enhancing Bioavailability in Drug Delivery)

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17 pages, 2291 KiB

Open AccessArticle

PEG-Modified tert-Octylcalix[8]arenes as Drug Delivery Nanocarriers of Silibinin

by Desislava Budurova, Denitsa Momekova, Georgi Momekov, Pavletta Shestakova, Hristo Penchev and Stanislav Rangelov

Pharmaceutics 2021, 13(12), 2025; https://doi.org/10.3390/pharmaceutics13122025 - 27 Nov 2021

Cited by 4 | Viewed by 1757

Abstract

The hepatoprotective properties of silibinin, as well its therapeutic potential as an anticancer and chemo-preventive agent, have failed to progress towards clinical development and commercialization due to this material’s unfavorable pharmacokinetics and physicochemical properties, low aqueous solubility, and chemical instability. The present contribution [...] Read more.

The hepatoprotective properties of silibinin, as well its therapeutic potential as an anticancer and chemo-preventive agent, have failed to progress towards clinical development and commercialization due to this material’s unfavorable pharmacokinetics and physicochemical properties, low aqueous solubility, and chemical instability. The present contribution is focused on the feasibility of using PEGylated calixarene, in particular polyoxyethylene-derivatized tert-octylcalix[8]arene, to prepare various platforms for the delivery of silibinin, such as inclusion complexes and supramolecular aggregates thereof. The inclusion complex is characterized by various instrumental methods. At concentrations exceeding the critical micellization concentration of PEGylated calixarene, the tremendous solubility increment of silibinin is attributed to the additional solubilization and hydrophobic non-covalent interactions of the drug with supramolecular aggregates. PEG-modified tert-octylcalix[8]arenes, used as drug delivery carriers for silibinin, were additionally investigated for cytotoxicity against human tumor cell lines. Full article

(This article belongs to the Special Issue Polymers Enhancing Bioavailability in Drug Delivery)

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16 pages, 3202 KiB

Open AccessArticle

Optimization and Development of Selective Histone Deacetylase Inhibitor (MPT0B291)-Loaded Albumin Nanoparticles for Anticancer Therapy

by Athika Darumas Putri, Pai-Shan Chen, Yu-Lin Su, Jia-Pei Lin, Jing-Ping Liou and Chien-Ming Hsieh

Pharmaceutics 2021, 13(10), 1728; https://doi.org/10.3390/pharmaceutics13101728 - 19 Oct 2021

Cited by 9 | Viewed by 2964

Abstract

Histone deacetylase (HDAC) inhibitors have emerged as a new class of antitumor agent for various types of tumors. MPT0B291, a novel selective inhibitor of HDAC6, demonstrated significant antiproliferative activity in various human cancer cell types. However, MPT0B291 has very low water solubility, which [...] Read more.

Histone deacetylase (HDAC) inhibitors have emerged as a new class of antitumor agent for various types of tumors. MPT0B291, a novel selective inhibitor of HDAC6, demonstrated significant antiproliferative activity in various human cancer cell types. However, MPT0B291 has very low water solubility, which limits its clinical use for cancer therapy. In the current study, MPT0B291 was encapsulated in human serum albumin (HSA), and its anticancer activities were investigated. Nanoparticles (NPs) were prepared using two-stage emulsification resulting in 100~200-nm NPs with a fine size distribution (polydispersity index of <0.3). The in vitro drug release profiles of MPT0B291-loaded HSA NPs presented sustained-release properties. The cytotoxic effect on MIA PaCa-2 human pancreatic carcinoma cells was found to be similar to MPT0B291-loaded HSA NPs and the free-drug group. The albumin-based formulation provided a higher maximum tolerated dose than that of a drug solution with reduced toxicity toward normal cells. Furthermore, in vivo pharmacokinetic studies demonstrated an effective increase (5~8-fold) in the bioavailability of NPs containing MPT0B291 loaded in HSA compared to the free-drug solution with an extended circulation time (t_1/2) leading to significantly enhanced efficacy of anticancer treatment. Full article

(This article belongs to the Special Issue Polymers Enhancing Bioavailability in Drug Delivery)

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18 pages, 2598 KiB

Open AccessArticle

Dual-Acting Zeta-Potential-Changing Micelles for Optimal Mucus Diffusion and Enhanced Cellular Uptake after Oral Delivery

by Ahmad Malkawi, Nasr Alrabadi and Ross Allan Kennedy

Pharmaceutics 2021, 13(7), 974; https://doi.org/10.3390/pharmaceutics13070974 - 27 Jun 2021

Cited by 5 | Viewed by 3082

Abstract

Context: Overcoming the intestinal mucosal barrier can be a challenge in drug delivery. Nanoemulsions with negative zeta potentials can effectively permeate the mucus layer, but those with positive zeta potentials are better taken up by cells; a nanoemulsion with capricious zeta potential from [...] Read more.

Context: Overcoming the intestinal mucosal barrier can be a challenge in drug delivery. Nanoemulsions with negative zeta potentials can effectively permeate the mucus layer, but those with positive zeta potentials are better taken up by cells; a nanoemulsion with capricious zeta potential from negative to positive can achieve both good permeation and high uptake. Objective: This study aimed to develop dual-acting zeta-potential-amphoteric micelles enabling optimal muco-permeation and enhancement of cellular uptake. Methods: A micellar pre-concentrate was prepared from 15% Labrasol, 15% Kolliphor EL, 30% Kolliphor RH 40, and 40% dimethylsulfoxide. The micellar pre-concentrate was loaded with anionic stearic acid (SA), forming ionic complexes with cationic polymers at a ratio of 25:1 with Eudragit RS 100 and Eudragit RL 100. Blank micelles and those containing complexes were separately diluted in physiological buffers and examined for their droplet sizes, polydispersity indices (PDIs), zeta potentials, and cytotoxicity. The SA release from the micellar complexes was evaluated in 0.1 mM phosphate buffer (pH 6.8) containing 0.001% fluorescein, thereby enabling an instant decrease in fluorescence. Finally, the micelles were loaded with the model drug fluorescein diacetate (FDA) and evaluated for their muco-permeation behavior and cellular uptake. Results: The micellar dilutions formed micelles at the critical micelle concentration (CMC) of 312 µg/mL and showed a uniform average droplet size of 14.2 nm, with a PDI < 0.1. Micellar dilutions were non-cytotoxic when used at 1:100 in a physiological medium. Micelles loaded with ionic complexes achieved a sustained release of 95.5 ± 3.7% of the SA in 180 min. Moreover, the zeta potential of the complex-loaded micelles shifted from −5.4 to +1.8 mV, whereas the blank micelles showed a stabilized zeta potential of −10 mV. Furthermore, the negatively charged blank and complex-loaded micelles exhibited comparable muco-permeation, with an overall average of 58.2 ± 3.7% diffusion of FDA. The complex-loaded micellar droplets, however, provided a significantly higher cellular uptake of the model drug FDA (2.2-fold, p ≤ 0.01) Conclusion: Due to undergoing a shift in zeta potential, the modified micelles significantly enhanced cellular uptake while preserving mucus-permeating properties. Full article

(This article belongs to the Special Issue Polymers Enhancing Bioavailability in Drug Delivery)

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12 pages, 19996 KiB

Open AccessArticle

The Preparation of a Novel Poly(Lactic Acid)-Based Sustained H₂S Releasing Microsphere for Rheumatoid Arthritis Alleviation

by Yue Yu, Zhou Wang, Qian Ding, Xiangbin Yu, Qinyan Yang, Ran Wang, Yudong Fang, Wei Qi, Junyi Liao, Wei Hu and Yizhun Zhu

Pharmaceutics 2021, 13(5), 742; https://doi.org/10.3390/pharmaceutics13050742 - 18 May 2021

Cited by 11 | Viewed by 2585

Abstract

Rheumatoid arthritis (RA) is a chronic, inflammatory autoimmune disease that mainly erodes joints and surrounding tissues, and if it is not treated in time, it can cause joint deformities and loss of function. S-propargyl-cysteine (SPRC) is an excellent endogenous hydrogen sulfide donor which [...] Read more.

Rheumatoid arthritis (RA) is a chronic, inflammatory autoimmune disease that mainly erodes joints and surrounding tissues, and if it is not treated in time, it can cause joint deformities and loss of function. S-propargyl-cysteine (SPRC) is an excellent endogenous hydrogen sulfide donor which can relieve the symptoms of RA through the promotion of H₂S release via the CSE/H₂S pathway in vivo. However, the instant release of H₂S in vivo could potentially limit its further clinical use. To solve this problem, in this study, a SPRC-loaded poly(lactic acid) (PLA) microsphere (SPRC@PLA) was prepared, which could release SPRC in vitro in a sustained manner, and further promote sustained in vivo H₂S release. Furthermore, its therapeutical effect on RA in rats was also studied. A spherical-like SPRC@PLA was successfully prepared with a diameter of approximately 31.61 μm, yielding rate of 50.66%, loading efficiency of 6.10% and encapsulation efficiency of 52.71%. The SPRC@PLA showed significant prolonged in vitro SPRC release, to 4 days, and additionally, an in vivo H₂S release around 3 days could also be observed. In addition, a better therapeutical effect and prolonged administration interval toward RA rats was also observed in the SPRC@PLA group. Full article

(This article belongs to the Special Issue Polymers Enhancing Bioavailability in Drug Delivery)

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20 pages, 3577 KiB

Open AccessArticle

Synthesis and Evaluation of Thiol-Conjugated Poloxamer and Its Pharmaceutical Applications

by Muhammad Zaman, Sadaf Saeed, Rabia Imtiaz Bajwa, Muhammad Shafeeq Ur Rahman, Saeed Ur Rahman, Muhammad Jamshaid, Muhammad F. Rasool, Abdul Majeed, Imran Imran, Faleh Alqahtani, Sultan Alshehri, Abdullah F. AlAsmari, Nemat Ali and Mohammed Alasmari

Pharmaceutics 2021, 13(5), 693; https://doi.org/10.3390/pharmaceutics13050693 - 11 May 2021

Cited by 2 | Viewed by 2630

Abstract

The current study was designed to convert the poloxamer (PLX) into thiolated poloxamer (TPLX), followed by its physicochemical, biocompatibilities studies, and applications as a pharmaceutical excipient in the development of tacrolimus (TCM)-containing compressed tablets. Thiolation was accomplished by using thiourea as a thiol [...] Read more.

The current study was designed to convert the poloxamer (PLX) into thiolated poloxamer (TPLX), followed by its physicochemical, biocompatibilities studies, and applications as a pharmaceutical excipient in the development of tacrolimus (TCM)-containing compressed tablets. Thiolation was accomplished by using thiourea as a thiol donor and hydrochloric acid (HCl) as a catalyst in the reaction. Both PLX and TPLX were evaluated for surface morphology based on SEM, the crystalline or amorphous nature of the particles, thiol contents, micromeritics, FTIR, and biocompatibility studies in albino rats. Furthermore, the polymers were used in the development of compressed tablets. Later, they were also characterized for thickness, diameter, hardness, weight variation, swelling index, disintegration time, mucoadhesion, and in vitro drug release. The outcomes of the study showed that the thiolation process was accomplished successfully, which was confirmed by FTIR, where a characteristic peak was noticed at 2695.9968 cm⁻¹ in the FTIR scan of TPLX. Furthermore, the considerable concentration of the thiol constituents (20.625 µg/g of the polymer), which was present on the polymeric backbone, also strengthened the claim of successful thiolation. A mucoadhesion test illustrated the comparatively better mucoadhesion strength of TPLX compared to PLX. The in vitro drug release study exhibited that the TPLX-based formulation showed a more rapid (p < 0.05) release of the drug in 1 h compared to the PLX-based formulation. The in vivo toxicity studies confirmed that both PLX and TPLX were safe when they were administered to the albino rats. Conclusively, the thiolation of PLX made not only the polymer more mucoadhesive but also capable of improving the dissolution profile of TCM. Full article

(This article belongs to the Special Issue Polymers Enhancing Bioavailability in Drug Delivery)

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18 pages, 4369 KiB

Open AccessArticle

The Impact of an Efflux Pump Inhibitor on the Activity of Free and Liposomal Antibiotics against Pseudomonas aeruginosa

by Douweh Leyla Gbian and Abdelwahab Omri

Pharmaceutics 2021, 13(4), 577; https://doi.org/10.3390/pharmaceutics13040577 - 18 Apr 2021

Cited by 11 | Viewed by 2468

Abstract

The eradication of Pseudomonas aeruginosa in cystic fibrosis patients has become continuously difficult due to its increased resistance to treatments. This study assessed the efficacy of free and liposomal gentamicin and erythromycin, combined with Phenylalanine arginine beta-naphthylamide (PABN), a broad-spectrum efflux pump inhibitor, [...] Read more.

The eradication of Pseudomonas aeruginosa in cystic fibrosis patients has become continuously difficult due to its increased resistance to treatments. This study assessed the efficacy of free and liposomal gentamicin and erythromycin, combined with Phenylalanine arginine beta-naphthylamide (PABN), a broad-spectrum efflux pump inhibitor, against P. aeruginosa isolates. Liposomes were prepared and characterized for their sizes and encapsulation efficiencies. The antimicrobial activities of formulations were determined by the microbroth dilution method. Their activity on P. aeruginosa biofilms was assessed, and the effect of sub-inhibitory concentrations on bacterial virulence factors, quorum sensing (QS) signals and bacterial motility was also evaluated. The average diameters of liposomes were 562.67 ± 33.74 nm for gentamicin and 3086.35 ± 553.95 nm for erythromycin, with encapsulation efficiencies of 13.89 ± 1.54% and 51.58 ± 2.84%, respectively. Liposomes and PABN combinations potentiated antibiotics by reducing minimum inhibitory and bactericidal concentrations by 4–32 fold overall. The formulations significantly inhibited biofilm formation and differentially attenuated virulence factor production as well as motility. Unexpectedly, QS signal production was not affected by treatments. Taken together, the results indicate that PABN shows potential as an adjuvant of liposomal macrolides and aminoglycosides in the management of lung infections in cystic fibrosis patients. Full article

(This article belongs to the Special Issue Polymers Enhancing Bioavailability in Drug Delivery)

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Review

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22 pages, 3407 KiB

Open AccessReview

Recent Advances in Hydrogel-Mediated Nitric Oxide Delivery Systems Targeted for Wound Healing Applications

by Gina Tavares, Patrícia Alves and Pedro Simões

Pharmaceutics 2022, 14(7), 1377; https://doi.org/10.3390/pharmaceutics14071377 - 29 Jun 2022

Cited by 13 | Viewed by 2573

Abstract

Despite the noticeable evolution in wound treatment over the centuries, a functional material that promotes correct and swift wound healing is important, considering the relative weight of chronic wounds in healthcare. Difficult to heal in a fashionable time, chronic wounds are more prone [...] Read more.

Despite the noticeable evolution in wound treatment over the centuries, a functional material that promotes correct and swift wound healing is important, considering the relative weight of chronic wounds in healthcare. Difficult to heal in a fashionable time, chronic wounds are more prone to infections and complications thereof. Nitric oxide (NO) has been explored for wound healing applications due to its appealing properties, which in the wound healing context include vasodilation, angiogenesis promotion, cell proliferation, and antimicrobial activity. NO delivery is facilitated by molecules that release NO when prompted, whose stability is ensured using carriers. Hydrogels, popular materials for wound dressings, have been studied as scaffolds for NO storage and delivery, showing promising results such as enhanced wound healing, controlled and sustained NO release, and bactericidal properties. Systems reported so far regarding NO delivery by hydrogels are reviewed. Full article

(This article belongs to the Special Issue Polymers Enhancing Bioavailability in Drug Delivery)

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27 pages, 3608 KiB

Open AccessReview

Polymer-Modified Liposomes for Drug Delivery: From Fundamentals to Applications

by Yifeng Cao, Xinyan Dong and Xuepeng Chen

Pharmaceutics 2022, 14(4), 778; https://doi.org/10.3390/pharmaceutics14040778 - 02 Apr 2022

Cited by 31 | Viewed by 6276

Abstract

Liposomes are highly advantageous platforms for drug delivery. To improve the colloidal stability and avoid rapid uptake by the mononuclear phagocytic system of conventional liposomes while controlling the release of encapsulated agents, modification of liposomes with well-designed polymers to modulate the physiological, particularly [...] Read more.

Liposomes are highly advantageous platforms for drug delivery. To improve the colloidal stability and avoid rapid uptake by the mononuclear phagocytic system of conventional liposomes while controlling the release of encapsulated agents, modification of liposomes with well-designed polymers to modulate the physiological, particularly the interfacial properties of the drug carriers, has been intensively investigated. Briefly, polymers are incorporated into liposomes mainly using “grafting” or “coating”, defined according to the configuration of polymers at the surface. Polymer-modified liposomes preserve the advantages of liposomes as drug-delivery carriers and possess specific functionality from the polymers, such as long circulation, precise targeting, and stimulus-responsiveness, thereby resulting in improved pharmacokinetics, biodistribution, toxicity, and therapeutic efficacy. In this review, we summarize the progress in polymer-modified liposomes for drug delivery, focusing on the change in physiological properties of liposomes and factors influencing the overall therapeutic efficacy. Full article

(This article belongs to the Special Issue Polymers Enhancing Bioavailability in Drug Delivery)

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22 pages, 1125 KiB

Open AccessReview

Potential Applications of Chitosan-Based Nanomaterials to Surpass the Gastrointestinal Physiological Obstacles and Enhance the Intestinal Drug Absorption

by Nutthapoom Pathomthongtaweechai and Chatchai Muanprasat

Pharmaceutics 2021, 13(6), 887; https://doi.org/10.3390/pharmaceutics13060887 - 15 Jun 2021

Cited by 27 | Viewed by 3603

Abstract

The small intestine provides the major site for the absorption of numerous orally administered drugs. However, before reaching to the systemic circulation to exert beneficial pharmacological activities, the oral drug delivery is hindered by poor absorption/metabolic instability of the drugs in gastrointestinal (GI) [...] Read more.

The small intestine provides the major site for the absorption of numerous orally administered drugs. However, before reaching to the systemic circulation to exert beneficial pharmacological activities, the oral drug delivery is hindered by poor absorption/metabolic instability of the drugs in gastrointestinal (GI) tract and the presence of the mucus layer overlying intestinal epithelium. Therefore, a polymeric drug delivery system has emerged as a robust approach to enhance oral drug bioavailability and intestinal drug absorption. Chitosan, a cationic polymer derived from chitin, and its derivatives have received remarkable attention to serve as a promising drug carrier, chiefly owing to their versatile, biocompatible, biodegradable, and non-toxic properties. Several types of chitosan-based drug delivery systems have been developed, including chemical modification, conjugates, capsules, and hybrids. They have been shown to be effective in improving intestinal assimilation of several types of drugs, e.g., antidiabetic, anticancer, antimicrobial, and anti-inflammatory drugs. In this review, the physiological challenges affecting intestinal drug absorption and the effects of chitosan on those parameters impacting on oral bioavailability are summarized. More appreciably, types of chitosan-based nanomaterials enhancing intestinal drug absorption and their mechanisms, as well as potential applications in diabetes, cancers, infections, and inflammation, are highlighted. The future perspective of chitosan applications is also discussed. Full article

(This article belongs to the Special Issue Polymers Enhancing Bioavailability in Drug Delivery)

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