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Ashish Kumar Jain*, Sunil Kumar Jain

Adina Institute of Pharmaceutical Sciences, Sagar, 470002, (M.P), India.


An objective of the present investigation was to prepare and evaluate PVP: PAA mucoadhesive microspheres of nateglinide and evaluate for their Anti diabetic activity. PVP: PAA microspheres were prepared by interpolymer complexation and solvent diffusion method using different ratios of PVP (0.1 to 0.3 w/w) in polymer matrix, nateglinide (20 to 80% w/w), emulsifier concentration (0.5 to 2.0 w/v), Water: Oil phase ratio (1:1 to1:10), stirring speeds (300-600 rpm) and stirring speeds (1-4 hr). The yield of preparation and encapsulation efficiency was high for all PVP: PAA mucoadhesive microspheres. Microspheres prepared by using PVP: PAA ratio 0.2 to1 %w/w, stirring speed 600 rpm, and 1.5 % w/v concentration of emulsifying agent (span 80) and 1:5 Water :Oil phase ratio were selected as an optimized formulation. The optimized PVP: PAA mucoadhesive microspheres were evaluated for their surface morphology, particle size and size distribution, swellability, percentage drug entrapment and in vitro nateglinide release in SGF (pH 1.2), SIF (pH 6.8) and PBS (pH 7.4). The % Cumulative amount of drug release was found 87.4705.89% in SGF (pH 1.2), 93.6103.5% in SIF (pH 6.8) and 93.63.2% in PBS (pH 7.4) up to 24 hrs. The data of drug released revealed that the microspheres formulation follows a diffusion controlled drug release mechanism. In vivo evaluation of the optimized PAA-PVP microspheres were carried out in healthy male albino rats by measuring hypoglycemic effect produced after oral administration at a dose (equivalent to 10 mg /kg b.w.of nateglinide). The progressive reduction in blood glucose level was observed till the end of study and maximum reduction (57.992.865 %) was achieved after 24 hrs. It is concluded from the present investigation that PVP: PAA mucoadhesive microspheres bearing nateglinide are promising controlled release vector for management of diabetes.

Keywords: PVP: PAA, mucoadhesive microspheres, Anti diabetic activity, Controlled release microspheres, nateglinide.

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