Enhancement of antiproliferative potential of metformin against melanoma mice B16 cells using an optimized liposomal drug delivery system.

OBJECTIVE: Metformin-loaded liposomes were optimized for enhanced antiproliferative activity against melanoma. METHODS: Box-Behnken design and response surface methodology were employed to optimize entrapment efficiency, ex-vivo permeation and vesicle size. The optimized formulation was prepared by both the lipid hydration method and the modified injection method for comparison. Different concentrations of Pluronic F127 were employed for modification. Selected Pluronic-modified formulation (lipid molar concentration 55 mmol, cholesterol 30% and drug loading 52.9 mg) was characterized for morphology, entrapment efficiency, permeation and vesicle size. RESULTS: The optimized formulation resulted in entrapment efficiency of 41.7 ± 0.01%, vesicle size of 1.405 ± 0.061 µm and percentage of permeation was 67 ± 5.5%. The improved cytotoxic effect of the selected formulation against melanoma mice B16 cell line compared with metformin solution was determined using MTT assay. Compared with the corresponding drug solution, the Pluronic-modified optimized liposomes displayed a highly efficient cytotoxic effect as evidenced by significant lowering in IC50 -887.3 ± 23.2 and 26.71 ± 0.69 µg/ml, respectively, P < 0.0001. CONCLUSION: This study introduces an optimized liposomal formulation with enhanced cytotoxic effect against melanoma B16 cell line.

Quercetin loaded cosm-nutraceutical electrospun composite nanofibers for acne alleviation: Preparation, characterization and experimental clinical appraisal.

In the cosmeceutical field, it is essential to develop topical delivery systems which would allow drugs to create a depot and permeate within the skin. The aim of the present study was to develop composite nanofibers of polyvinyl alcohol/quercetin/essential oils using the electrospinning technique, and assess their efficiency in acne alleviation. Quercetin was chosen due to its anti-inflammatory, anti-oxidant, and antibacterial activities. Nanofibers were characterized for their morphology, ex-vivo deposition/permeation, physical/mechanical integrity, thermal properties, and chemical characteristics. In addition, the anti-bacterial efficacy was tested on Propionibacterium acne (P. acne), and a cytotoxicity assay was carried out. Lastly, an experimental clinical trial was conducted on acne patients, where the percentage reduction of inflammatory, non-inflammatory and total acne lesions was taken as evaluation criterion. Results showed that quercetin was successfully loaded into the nanofibers which were homogenously dispersed. They showed a reasonable skin deposition percentage of 28.24% ± 0.012, a significantly higher antibacterial efficacy against Propionibacterium acne than quercetin alone, and were utterly safe on skin fibroblastic cells. Upon clinical examination on acne patients, the nanofibers showed 61.2%, 14.7%, and 52.9% reduction of inflammatory, comedonal, and total acne lesions respectively, suggesting a promising topical anti-acne delivery system.

Chitosan nanoparticles making their way to clinical practice: A feasibility study on their topical use for acne treatment.

Despite the popularity of chitosan as a biodegradable polymer used in a variety of applications, clinical trials involving chitosan or its nanoparticles are still scarce. Moreover, the use of nutraceuticals as a replacement to conventional chemical treatments has become currently popular, and if combined with nanotechnology, nutraceuticals can achieve a comparable or even better therapeutic outcome. In the current work, chitosan nanoparticles loading the nutraceutical nicotinamide were optimized, characterized, and clinically tested on patients suffering from acne vulgaris. The topical merits of chitosan nanoparticles were proven, in which they exhibited strong skin adhesion ex vivo and high nicotinamide deposition in the different skin layers (stratum corneum, epidermis and dermis) amounting to a total of 68%. When clinically tested on patients, nicotinamide nanoparticles displayed 73% reduction in the inflammatory acne lesions compared to untreated areas, hence proving that chitosan nanoparticles can be a clinically sounding option for treatment of skin diseases.

Novel nicotinamide skin-adhesive hot melt extrudates for treatment of acne.

OBJECTIVES: Hot melt extrusion is a continuous process with wide industrial applicability. Till current date, there have been no reports on the formulation of extrudates for topical treatment of dermatological diseases. METHODS: The aim of the present work was to prepare and characterize medicated hot melt extrudates based on Soluplus polymer and nicotinamide, and to explore their applicability in acne treatment. The extrudates were characterized using DSC, FTIR, XRD, and DVS. The extrudates were also tested for their skin adhesion potential, ability to deposit nicotinamide in different skin layers, and their clinical efficacy in acne patients. RESULTS: The 10% nicotinamide extrudates exhibited amorphous nature which was reserved during storage, with no chemical interaction between nicotinamide and Soluplus. Upon contrasting the skin adhesion and drug deposition of extrudates and nicotinamide gel, it was evident that the extrudates displayed significantly higher adhesion and drug deposition reaching 4.8 folds, 5.3 folds, and 4.3 folds more in the stratum corneum, epidermis and dermis, respectively. Furthermore, the extrudates significantly reduced the total number of acne lesions in patients by 61.3% compared to 42.14% with the nicotinamide gel. CONCLUSION: Soluplus extrudates are promising topical drug delivery means for the treatment of dermatological diseases.