Particle size

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.  

The objective of this study was to develop self-emulsifying drug delivery system (SEDDS) to enhance the solubility of the poorly water-soluble drug Orlistat. Orlistat is class II molecule according to BCS (Biopharmaceutical Classification System), having low solubility and low permeability. The rate and extent of absorption of class II compounds is highly dependent on the performance of the formulated product. These drugs can be successfully formulated for oral administration, but care needs to be taken with formulation design to ensure consistent bioavailability. Solubility of Orlistat was evaluated in various nonaqueous carriers that included oils, surfactants, and cosurfactants. Pseudoternary phase diagrams were constructed to identify the self-microemulsification region. Self microemulsifying formulations were prepared using mixtures of oils, surfactants, and cosurfactants in various proportions. The self microemulsification properties, droplet size and thermodynamic stability of these formulations were studied upon dilution with water. The optimized liquid SMEDDS formulation was converted into free flowing powder by adsorbing onto a solid carrier for encapsulation. The dissolution characteristics of solid intermediates of SMEDDS filled into hard gelatin capsules were investigated and compared with pure drug and commercial formulation. The results indicated that solid intermediates showed the rate and extent of drug dissolution for solid intermediates were significantly higher than commercial formulation. The results of the study demonstrated the potential use of SMEDDS as a means of improving solubility, dissolution and concomitantly the bioavailability.