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Open AccessArticle

Piperine-Loaded In Situ Gel: Formulation, In Vitro Characterization, and Clinical Evaluation against Periodontitis

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Poornima K. Gopalakrishna

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Rajamma Abburu Jayaramu

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Sateesha Shivally Boregowda

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Gels 2023, 9(7), 577; https://doi.org/10.3390/gels9070577 - 14 Jul 2023

Viewed by 506

Abstract

Periodontitis is an inflammatory disorder associated with dysbiosis and characterized by microbiologically related, host-mediated inflammation that leads to the damage of periodontal tissues including gingiva, connective tissues, and alveolar bone. The aim of this study was to develop an in situ gel consisting [...] Read more.

Periodontitis is an inflammatory disorder associated with dysbiosis and characterized by microbiologically related, host-mediated inflammation that leads to the damage of periodontal tissues including gingiva, connective tissues, and alveolar bone. The aim of this study was to develop an in situ gel consisting of piperine. Eight in situ gel formulations were designed by varying the concentration of deacylated gellan gum cross-linked with sodium tripolyphosphate, and poloxamer-407. The prepared gels were evaluated for gelation temperature, gelation time, viscosity, piperine-loading efficiency, and piperine release. Finally, the optimized formula was evaluated for anti-inflammatory effectiveness among human patients during a 14-day follow-up. The optimized in situ gel formulation exhibited a gelation temperature of 35 ± 1 °C, gelling of 36 ± 1 s, excellent syringeability, and piperine loading of 95.3 ± 2.3%. This formulation efficiently sustained in vitro drug release for up to 72 h. In vivo studies revealed an efficient sol-to-gel transformation of optimized in situ gel formulation at physiological conditions, permitting an efficient residence time of the formulation within a periodontitis pocket. Most importantly, a clinical study revealed that treatment with the optimized formulation elicited a significant reduction in the mean plaque score (p = 0.001), gingival index (p = 0.003), and pocket depth (p = 0.002), and exerted a potent anti-inflammatory potential, compared to the control group. Collectively, piperine-loaded in situ gel might represent a viable therapeutic approach for the management of gingival and periodontal diseases. Full article

(This article belongs to the Special Issue Design and Optimization of Pharmaceutical Gels)

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Open AccessArticle

Enhanced Osteogenesis Potential of MG-63 Cells through Sustained Delivery of VEGF via Liposomal Hydrogel

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Milton Hongli Tsai

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Rohaya Megat Abdul Wahab

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Shahrul Hisham Zainal Ariffin

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Fazren Azmi

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Farinawati Yazid

Gels 2023, 9(7), 562; https://doi.org/10.3390/gels9070562 - 10 Jul 2023

Cited by 1 | Viewed by 486

Abstract

The challenges of using VEGF to promote osteoblastic differentiation include a short half-life and a narrow therapeutic window. A carrier system combining hydrogel and liposomes may improve the therapeutic efficacy of VEGF for bone regeneration. This study aimed to investigate the effects of [...] Read more.

The challenges of using VEGF to promote osteoblastic differentiation include a short half-life and a narrow therapeutic window. A carrier system combining hydrogel and liposomes may improve the therapeutic efficacy of VEGF for bone regeneration. This study aimed to investigate the effects of delivery of VEGF via liposomal hydrogel on the osteogenesis of MG-63 cells. Liposomal hydrogel scaffold was fabricated and then characterized in terms of the morphological and chemical properties using FESEM and FTIR. In 2.5D analysis, the MG-63 cells were cultured on liposomal hydrogel + VEGF as the test group. The osteogenic effects of VEGF were compared with the control groups, i.e., hydrogel without liposomes + VEGF, osteogenic medium (OM) supplemented with a bolus of VEGF, and OM without VEGF. Cell morphology, viability, and differentiation and mineralization potential were investigated using FESEM, MTT assay, ALP activity, and Alizarin red staining. The characterization of scaffold showed no significant differences in the morphological and chemical properties between hydrogel with and without liposomes (p > 0.05). The final 2.5D culture demonstrated that cell proliferation, differentiation, and mineralization were significantly enhanced in the liposomal hydrogel + VEGF group compared with the control groups (p < 0.05). In conclusion, liposomal hydrogel can be used to deliver VEGF in a sustained manner in order to enhance the osteogenesis of MG-63 cells. Full article

(This article belongs to the Special Issue Design and Optimization of Pharmaceutical Gels)

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Open AccessArticle

Numerical Optimization of Prednisolone–Tacrolimus Loaded Ultraflexible Transethosomes for Transdermal Delivery Enhancement; Box–Behnken Design, Evaluation, Optimization, and Pharmacokinetic Study

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Munerah M. Alfadhel

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Randa Mohammed Zaki

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Basmah Nasser Aldosari

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Ossama M. Sayed

Gels 2023, 9(5), 400; https://doi.org/10.3390/gels9050400 - 10 May 2023

Viewed by 848

Abstract

The aim of the present study is to formulate highly permeable carriers (i.e., transethosomes) for enhancing the delivery of prednisolone combined with tacrolimus for both topical and systemic pathological conditions. A Box–Behnken experimental design was implemented in this research. Three independent variables: surfactant [...] Read more.

The aim of the present study is to formulate highly permeable carriers (i.e., transethosomes) for enhancing the delivery of prednisolone combined with tacrolimus for both topical and systemic pathological conditions. A Box–Behnken experimental design was implemented in this research. Three independent variables: surfactant concentration (X1), ethanol concentration (X2), and tacrolimus concentration (X3) were adopted in the design while three responses: entrapment efficiency (Y1), vesicle size (Y2), and zeta potential (Y3) were investigated. By applying design analysis, one optimum formulation was chosen to be incorporated into topical gel formulation. The optimized transethosomal gel formula was characterized in terms of pH, drug content, and spreadability. The gel formula was challenged in terms of its anti-inflammatory effect and pharmacokinetics against oral prednisolone suspension and topical prednisolone–tacrolimus gel. The optimized transethosomal gel achieved the highest rate of rat hind paw edema reduction (98.34%) and highest pharmacokinetics parameters (Cmax 133.266 ± 6.469 µg/mL; AUC_0-∞ 538.922 ± 49.052 µg·h/mL), which indicated better performance of the formulated gel. Full article

(This article belongs to the Special Issue Design and Optimization of Pharmaceutical Gels)

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Open AccessArticle

Emulsion-Based Gel Loaded with Ibuprofen and Its Derivatives

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Adebukola Abiola Agboola

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Adrian Krzysztof Antosik

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Paula Ossowicz-Rupniewska

Gels 2023, 9(5), 391; https://doi.org/10.3390/gels9050391 - 08 May 2023

Viewed by 723

Abstract

The aim of this study was to evaluate the effect of vehicle and chemical modifications of the structure of active compounds on the skin permeation and accumulation of ibuprofen (IBU). As a result, semi-solid formulations in the form of an emulsion-based gel loaded [...] Read more.

The aim of this study was to evaluate the effect of vehicle and chemical modifications of the structure of active compounds on the skin permeation and accumulation of ibuprofen (IBU). As a result, semi-solid formulations in the form of an emulsion-based gel loaded with ibuprofen and its derivatives, such as sodium ibuprofenate (IBUNa) and L-phenylalanine ethyl ester ibuprofenate ([PheOEt][IBU]), were developed. The properties of the obtained formulations were examined, including density, refractive index, viscosity, and particle size distribution. The parameters of release and permeability through the pig skin of the active substances contained in the obtained semi-solid formulations were determined. The results indicate that an emulsion-based gel enhanced the skin penetration of IBU and its derivatives compared to two commercial preparations in the form of a gel and a cream. The average cumulative mass of IBU after a 24 h permeation test from an emulsion-based gel formulation through human skin was 1.6–4.0 times higher than for the commercial products. Ibuprofen derivatives were evaluated as chemical penetration enhancers. After 24 h of penetration, the cumulative mass was 1086.6 ± 245.8 for IBUNa and 948.6 ± 87.5 µg IBU/cm² for [PheOEt][IBU], respectively. This study demonstrates the perspective of the transdermal emulsion-based gel vehicle in conjunction with the modification of the drug as a potentially faster drug delivery system. Full article

(This article belongs to the Special Issue Design and Optimization of Pharmaceutical Gels)

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Open AccessArticle

Response Surface Methodology for Optimization of Hydrogel-Forming Microneedles as Rapid and Efficient Transdermal Microsampling Tools

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Jiraporn Leanpolchareanchai

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Nantana Nuchtavorn

Gels 2023, 9(4), 306; https://doi.org/10.3390/gels9040306 - 06 Apr 2023

Cited by 1 | Viewed by 892

Abstract

Microneedles (MNs) have shown a great potential for the microsampling of dermal interstitial fluid (ISF) in a minimally invasive manner for point-of-care testing (POCT). The swelling properties of hydrogel-forming microneedles (MNs) allow for passive extraction of ISF. Surface response approaches, including Box-Behnken design [...] Read more.

Microneedles (MNs) have shown a great potential for the microsampling of dermal interstitial fluid (ISF) in a minimally invasive manner for point-of-care testing (POCT). The swelling properties of hydrogel-forming microneedles (MNs) allow for passive extraction of ISF. Surface response approaches, including Box-Behnken design (BBD), central composite design (CCD), and optimal discrete design, were employed for the optimization of hydrogel film by studying the effects of independent variables (i.e., the amount of hyaluronic acid, Gantrez^TM S-97, and pectin) on the swelling property. The optimal discrete model was selected to predict the appropriate variables, due to the good fit of the experimental data and the model validity. The analysis of variance (ANOVA) of the model demonstrated p-value < 0.0001, R² = 0.9923, adjusted R² = 0.9894, and predicted R² = 0.9831. Finally, the predicted film formulation containing 2.75% w/w hyaluronic acid, 1.321% w/w Gantrez^TM S-97, and 1.246% w/w pectin was used for further fabrication of MNs (525.4 ± 3.8 µm height and 157.4 ± 2.0 µm base width), which possessed 1508.2 ± 66.2% swelling, with 124.6 ± 7.4 µL of collection volume, and could withstand thumb pressure. Moreover, almost 50% of MNs achieved a skin insertion depth of approx. 400 µm, with 71.8 ± 3.2% to 78.3 ± 2.6% recoveries. The developed MNs show a promising prospect in microsample collection, which would be beneficial for POCT. Full article

(This article belongs to the Special Issue Design and Optimization of Pharmaceutical Gels)

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Open AccessArticle

Design and Evaluation of Paeonol-Loaded Liposomes in Thermoreversible Gels for Atopic Dermatitis

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Gels 2023, 9(3), 198; https://doi.org/10.3390/gels9030198 - 05 Mar 2023

Cited by 1 | Viewed by 957

Abstract

Paeonol (PAE) is a hydrophobic drug. In this study, we encapsulated paeonol in a lipid bilayer of liposomes (PAE-L), which delayed drug release and increased drug solubility. When PAE-L was dispersed in gels (PAE-L-G) based on a poloxamer matrix material for local transdermal [...] Read more.

Paeonol (PAE) is a hydrophobic drug. In this study, we encapsulated paeonol in a lipid bilayer of liposomes (PAE-L), which delayed drug release and increased drug solubility. When PAE-L was dispersed in gels (PAE-L-G) based on a poloxamer matrix material for local transdermal delivery, we observed amphiphilicity, reversible thermal responsiveness, and micellar self-assembly behavior. These gels can be used for atopic dermatitis (AD), an inflammatory skin disease, to change the surface temperature of the skin. In this study, we prepared PAE-L-G at an appropriate temperature for the treatment of AD. We then assessed the gel’s relevant physicochemical properties, in vitro cumulative drug release, and antioxidant properties. We found that PAE-loaded liposomes could be designed to increase the drug effect of thermoreversible gels. At 32 °C, PAE-L-G could change from solution state to gelatinous state at 31.70 ± 0.42 s, while the viscosity was 136.98 ± 0.78 MPa.S and the free radical scavenging rates on DPPH and H₂O₂ were 92.24 ± 5.57% and 92.12 ± 2.71%, respectively. Drug release across the extracorporeal dialysis membrane reached 41.76 ± 3.78%. In AD-like mice, PAE-L-G could also relieve skin damage by the 12th day. In summary, PAE-L-G could play an antioxidant role and relieve inflammation caused by oxidative stress in AD. Full article

(This article belongs to the Special Issue Design and Optimization of Pharmaceutical Gels)

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Open AccessReview

Utilization of Lyotropic Liquid Crystalline Gels for Chronic Wound Management

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Gels 2023, 9(9), 738; https://doi.org/10.3390/gels9090738 - 12 Sep 2023

Viewed by 342

Abstract

Management of chronic wounds is becoming a serious health problem worldwide. To treat chronic wounds, a suitable healing environment and sustained delivery of growth factors must be guaranteed. Different therapies have been applied for the treatment of chronic wounds such as debridement and [...] Read more.

Management of chronic wounds is becoming a serious health problem worldwide. To treat chronic wounds, a suitable healing environment and sustained delivery of growth factors must be guaranteed. Different therapies have been applied for the treatment of chronic wounds such as debridement and photodynamic therapy. Among them, growth factors are widely used therapeutic drugs. However, at present, growth factor delivery systems cannot meet the demand of clinical practice; therefore new methods should be developed to meet the emerging need. For this reason, researchers have tried to modify hydrogels through some methods such as chemical synthesis and molecule modifications to enhance their properties. However, there are still a large number of limitations in practical use like byproduct problems, difficulty to industrialize, and instability of growth factor. Moreover, applications of new materials like lyotropic liquid crystalline (LLC) on chronic wounds have emerged as a new trend. The structure of LLC is endowed with many excellent properties including low cost, ordered structure, and excellent loading efficiency. LLC can provide a moist local environment for the wound, and its lattice structure can embed the growth factors in the water channel. Growth factor is released from the high-concentration carrier to the low-concentration release medium, which can be precisely regulated. Therefore, it can provide sustained and stable delivery of growth factors as well as a suitable healing environment for wounds, which is a promising candidate for chronic wound healing and has a broad prospective application. In conclusion, more reliable and applicable drug delivery systems should be designed and tested to improve the therapy and management of chronic wounds. Full article

(This article belongs to the Special Issue Design and Optimization of Pharmaceutical Gels)

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Open AccessReview

Enhancing Therapeutic Efficacy of Curcumin: Advances in Delivery Systems and Clinical Applications

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Hossein Omidian

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Renae L. Wilson

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Sumana Dey Chowdhury

Gels 2023, 9(8), 596; https://doi.org/10.3390/gels9080596 - 25 Jul 2023

Cited by 1 | Viewed by 654

Abstract

Curcumin, a potent active compound found in turmeric and Curcuma xanthorrhiza oil, possesses a wide range of therapeutic properties, including antibacterial, anti-inflammatory, antioxidant, and wound healing activities. However, its clinical effectiveness is hindered by its low bioavailability and rapid elimination from the body. [...] Read more.

Curcumin, a potent active compound found in turmeric and Curcuma xanthorrhiza oil, possesses a wide range of therapeutic properties, including antibacterial, anti-inflammatory, antioxidant, and wound healing activities. However, its clinical effectiveness is hindered by its low bioavailability and rapid elimination from the body. To overcome these limitations, researchers have explored innovative delivery systems for curcumin. Some promising approaches include solid lipid nanoparticles, nanomicelle gels, and transdermal formulations for topical drug delivery. In the field of dentistry, curcumin gels have shown effectiveness against oral disorders and periodontal diseases. Moreover, Pickering emulsions and floating in situ gelling systems have been developed to target gastrointestinal health. Furthermore, curcumin-based systems have demonstrated potential in wound healing and ocular medicine. In addition to its therapeutic applications, curcumin also finds use as a food dye, contraception aid, corrosion-resistant coating, and environmentally friendly stain. This paper primarily focuses on the development of gel compositions of curcumin to address the challenges associated with its clinical use. Full article

(This article belongs to the Special Issue Design and Optimization of Pharmaceutical Gels)

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