pH responsive cylindrical MSN for oral delivery of insulin-design, fabrication and evaluation.

OBJECTIVE

The objective of the present study was to develop novel PMV [poly (methacrylic acid-co-vinyl triethoxylsilane)]-coated mesoporous silica nanoparticles (MSN) with improved hypoglycemic effect for oral insulin (INS) delivery.

METHODS

MSN was synthesized under acidic condition using Pluronic® P 123 and Tetra ethoxy orthosilane. Surfactant was removed by calcination. Calcined MSN was coated with pH sensitive polymer PMV. Cytotoxicity of this coated MSN was evaluated by MTT assay using CHO-K1 cell line. Different MSN samples were characterized with BET surface area analyzer, FESEM, TEM, FT-IR, XRD, TG-DTA. In vivo study was performed using male rats. Pharmacokinetic study was conducted using HPLC.

RESULTS AND DISCUSSION: Highest surface area (304.3921 m2/g) was observed in case of calcined sample. Adsorption pore width of final coated sample was highest (64.7844 nm) compared with others. No noticeable cytotoxicity was observed for this coated support. The entrapment efficiency of insulin was found to be 39.39%. In vitro studies were done at different pH using Franz-diffusion cell. Results showed significant release at pH 7.4. Cumulative drug release over a period of 6 h was more than 48% at this systemic pH. Effect of this MSN-PMV-INS on blood glucose level was retained for 16 h. This novel formulation has shown 73.10% relative bioavailability of insulin.

CONCLUSION

A novel-coated mesoporous silica support was successfully developed for delivery of insulin through oral route.