Development of Microsponges for Topical Delivery of Mupirocin

The goal of the present study was to develop and evaluate microsponge-based topical delivery system of mupirocin for sustained release and enhanced drug deposition in the skin. Microsponges containing mupirocin were prepared by an emulsion solvent diffusion method. The effect of formulation and process variables such as internal phase volume and stirring speed on the physical characteristics of microsponges were examined on optimized drug/polymer ratio by 32 factorial design. The optimized microsponges were incorporated into an emulgel base. In vitro drug release, ex vivo drug deposition, and in vivo antibacterial activity of mupirocin-loaded formulations were studied. Developed microsponges were spherical and porous, and there was no interaction between drug and polymer molecules. Emulgels containing microsponges showed desired physical properties. Drug release through cellulose dialysis membrane showed diffusion-controlled release pattern and drug deposition studies using rat abdominal skin exhibited significant retention of active in skin from microsponge-based formulations by 24 h. The optimized formulations were stable and nonirritant to skin as demonstrated by Draize patch test. Microsponges-based emulgel formulations showed prolonged efficacy in mouse surgical wound model infected with S. aureus. Mupirocin was stable in topical emulgel formulations and showed enhanced retention in the skin indicating better potential of the delivery system for treatment of primary and secondary skin infections, such as impetigo, eczema, and atopic dermatitis

Preparation of Intravenous Stealthy Acyclovir Nanoparticles with Increased Mean Residence Time

A major cause of thromboplebitis, during acyclovir (ACV) parenteral administration is the high pH of its reconstituted solution (pH 11). Its plasma half life is 2.5 h, requiring repeated administration which may result in excess of drug solubility leading to possible renal damage and acute renal failure. The present study reports the efficiency of stealthy ACV nanoparticles (NPs) to increase the mean residence time of the drug 29 times. It caused a marked decrease in thrombophlebitis when injected into rabbit’s ear vein. The polymers used were (Poly lactic acid, polylactic-co-glycolic (PLGA) 85/15, PLGA 75/25, PLGA 50/50). Particles were evaluated for their encapsulation efficiency, morphology, particle size and size distribution, zeta potential, and in vitro drug release. Small NPs (280–300 nm) with 60% drug release after 48 h were obtained. Among the block copolymer used, poloxamer 407 was of superior coating properties with a coat thickness in the range of 1.5–8.3 nm and a decreased surface charge

Preparation and Evaluation of Tubular Micelles of Pluronic Lecithin Organogel for Transdermal Delivery of Sumatriptan

The present work focuses on the preparation and evaluation of lecithin organogel system of thermoreversible polymer pluronic F127, which would enhance the stability and absorption of sumatriptan succinate across the skin. Formulations were developed with and without co-surfactant (pluronic F127). The prepared organogels were evaluated for its appearance, organoleptic characteristics, and feel upon application, homogeneity, occlusivenes, washability, pH, viscosity, spreadability, gel transition temperature of formulations. The formulations were also evaluated for drug content, in vitro drug diffusion properties and skin irritation testing. In vivo evaluation of formulations was carried out by hot plate and writhing test method, and finally the optimized formulation was subjected to stability studies. The developed formulations were easily washable, smooth in feel, and showed no clogging which indicate superior texture of system. Formulation, containing pluronic showed greater spreadability and higher drug diffusion rate as compared to pluronic free organogel. Drug content of organogel formulations was in the range of 94–97%. The pH of the formulations was 6.48 ± 0.5 and 6.98 ± 0.1, reflecting no risk of skin irritation. Pluronic not only enhances the stability of organogel by increasing the viscosity (from 6,541 ± 234.76 to 7,826 ± 155.65 poise) but also increases the release of drug from 67.39 ± 1.53% to 74.21 ± 1.7%. The sumatriptan exhibits higher and long lasting antinociceptive effect as indicated by the persistent increase in reaction time in hot plate and inhibited abdominal contraction in acetic acid-induced writhing test (p < 0.05). The prepared optimized formulation was found to be stable without any significant changes at room temperature