Microsponges

Controlled topical release drug delivery system for Fluconazole  is potentially useful in improving drug deposition in the skin and reducing the incidence of adverse side effects. The purpose of the present experiment was to produce a topical gel system for the delivery of . Drug loaded microsponges (1–10) were formulated by an emulsion solvent diffusion method. Optimization of the microsponges was selected by drug loading efficiency. The optimized microsponges was formulated as topical gel and evaluated. The in vitro drug release, ex vivo drug deposition, primary skin irritancy study and in vivo antibacterial activity of  loaded formulations were studied. The spherical and porous microparticles were obtained. Moreover, the optimized microsponge possess particle size, entrapment efficiency and production yield and of 84.49 µm, 72.21% and 39.40% respectively. Microsponge loaded gels indicated controlled release, no irritancy to rat skin and antifungal activity. An in vivo skin deposition study proved three fold higher retention in the stratum corneum layer as compared with plain  gel. Microsponges-based gel formulations showed prolonged efficacy in a rat surgical wound model infected with Candida albicans. These results suggest that was stable in topical formulations and amplifying retention in the skin, indicating better potential of the delivery system for treatment of primary and secondary skin infections. Keywords: Microsponges, Particle size, Entrapment efficiency, Primary skin irritancy, in vivo skin deposition Candida albicans.  

Microsponges are tiny, uniform, micro-porous polymeric beads and spherical in shape. It has the interconnected voids. The particle size of it ranges between 5-300μm. The porous surface of non-collapsible structure of microsponges helps to deliver the active ingredient in controlled manner. Diclofenac Sodium is a Non-steroidal anti-inflammatory drug. The plasma half-life of Diclofenac is 1-2 hrs which increases the dosing frequency and this drug also causes the gastrointestinal irritation. Therefore the purpose of present investigation was to design suitable controlled release Diclofenac Sodium microsponges which can reduce the dosing frequency and gastric irritation. In the present work, Diclofenac Sodium loaded eudragit microsponges were prepared using quasi emulsion solvent diffusion method. Different drug: polymer ratios were used to formulate the microsponges. The compatibility of the drug with polymer was established. Surface morphology of the microsponges was examined using scanning electron microscopy. Production yield, loading efficiency, particle size analysis, and in-vitro release studies were carried out. In-vitro release study showed that the release of drug was in controlled manner and it was increased with increase in drug to polymer ratio up to certain limit.

Over the past decade, numerous limitations of conventional dosage forms had attracted researchers to find a rational and appropriate drug delivery system. Microsponges were developed and studied as a novel programmable delivery system which is intended to deliver drug in controlled release pattern. It also aims epidermal localization of topical drug therapy to reduce their side effects by limiting systemic absorption through skin. Drug loaded microsponges are microporous beads, typically 10-25 µm in diameter which can entrap a wide variety of actives and can be formulated as creams, lotions, gels, ointments, powders, soaps. Microsponge formulations can increase product stability, enhance aesthetic qualities, and provide formulation flexibility and stability. Moreover, their non-antigenicity, non-toxicity, non-mutagenicity and non-biodegradability make them favourable candidates. Microsponge approach has also been applied in oral therapy, bone, tissue & cartilage engineering and showed remarkable results. This article provides description about the nature of microsponges, their characteristics, preparation, applications and commercial market status globally.