Design and characterization of enteric-coated controlled release mucoadhesive microcapsules of Rabeprazole sodium.

The objectives of present work was to design and characterize the rabeprazole sodium loaded microcapsules prepared by solvent evaporation technique using ethyl cellulose (EC) based various mucoadhesive polymer, followed by a triple coating with Eudragit L100. The Box-behnken design (BBD) was applied for optimization of formulations containing EC, HPMCK100M and Eudragit L100 as factors for selected responses like entrapment efficiency, mucoadhesive property and drug release in 24 h. The prepared microcapsules were characterized for particle size, drug content, swelling index, mucoadhesive strength, and in vivo antiulcer activity. FT-IR studies revealed that there was no drug-polymer interaction. SEM studies revealed that microcapsules were non-aggregated, spherical shape and smooth appearance. In vitro drug release data from microcapsules was fitted to different kinetic models to explain release profiles. The correlation coefficient value (r(2)) indicated that the drug release followed Higuchi model. Analysis of variance (ANOVA) showed significant difference in the release of drug from all formulations at p < 0.05 level. Accelerated stability study of optimized formulation (F4) upto 6 months showed there was no change in drug content and release characteristics during storage. In vivo antiulcer activity showed that the optimized microcapsules were able to protect rat stomach against ulcer formation vis-à-vis aqueous solution of the drug showed only negligible and minimum effect.

SEDDS Basic Design and Recent Formulation Advancement: A Concurrent Review.

In the present scenario, lipid-based novel drug delivery systems are the area of interest for the formulation scientist in order to improve the bioavailability of poorly water-soluble drugs. A selfemulsifying drug delivery system (SEDDS) upon contact with the gastrointestinal fluid, forms an o/w emulsion. SEDDS has gained popularity as a potential platform for improving the bioavailability of the lipophilic drug by overcoming several challenges. The various advantages like improved solubility, bypassing lymphatic transport, and improvement in bioavailability are associated with SMEDDS or SNEDDS. The extent of the formation of stable SEDDS depends on a specific combination of surfactant, co-surfactant, and oil. The present review highlighted the different aspects of formulation design along with optimization and characterization of SEDDS formulation. It also gives a brief description of the various aspects of the excipients used in SEDDS formulation. This review also includes the conflict between types of SEDDS based on droplet size. There is an extensive review of various research regarding different solidification techniques used for SEDDS in the last three years.

Formulation Design, Optimization and Pharmacodynamic Evaluation of Sustained Release Mucoadhesive Microcapsules of Venlafaxine HCl.

The objective of present research work was to design and characterize the venlafaxine HCl-loaded sodium alginate-based mucoadhesive microcapsules by ionic gelation technique using HPMC K100M as mucoadhesive polymer. The Placket-Burman Design was applied for preliminary screening of the formulations and systematic optimization by using Box-Behnken Design. The prepared microcapsules were characterized for drug content, entrapment efficiency, micromeritic properties, particle size, swelling index, mucoadhesive strength, in vitro drug release and in vivo antidepressant activity. FTIR and differential scanning calorimetry studies showed no incompatibility. Surface morphology studies revealed spherical nature of the prepared microcapsules. In vitro drug release studies revealed sustained release by diffusion mechanism. Further, the microcapsules were effective in reducing the depression induced by forced swimming test in Sprague-Dawley rats compared to the pure drug. The microcapsules were found to be stable under accelerated stability conditions, which suggest them as better alternative delivery systems for enhanced therapeutic efficacy of antidepressant drug, venlafaxine HCl.