NDLI: Influence of selected formulation variables on the preparation of enzyme-entrapped eudragit S100 microspheres

Content Provider	Springer Nature Link
Author	Rawat, Manju Saraf, Shailendra Saraf, Swarnlata
Copyright Year	2007
Abstract	The aim of this work is to study the influence of formulation parameters in the preparation of sustained release enzyme-loaded Eudragit S100 microspheres by emulsion solvent diffusion technique. A 3$^{2}$ full factorial experiment was designed to study the effects of the amount of solvent (dichloromethane) and stabilizers (Tween 20, 40, or 80) on the drug content and microsphere size. The results of analysis of variance test for both effects indicated that the test is significant. The effect of amount of stabilizer was found to be higher on both responses (SS$_{Y1}$=45.60; SS$_{Y2}$=737.93), whereas solvent concentration comparatively produced significant effect on the size of microspheres (SS$_{Y1}$=0.81; SS$_{Y2}$=358.83). Scanning electron microscopy of microspheres with maximum drug content (2.5 mL dichloromethane and 0.1 mL Tween 80) demonstrated smooth surface spherical particles with mean diameter of 56.83±2.88 µm. The effect of formulation variables on the integrity of enzyme was confirmed by in vitro proteolytic activity. The enteric nature of microspheres was evaluated and results demonstrated ∼6% to 7% release of enzyme in acidic medium. The release of enzyme from microspheres followed Higuchi kinetics. In phosphate buffer, microspheres showed an initial burst release of 20.34%±2.35% in 1 hour with additional 58.79%±4.32% release in the next 5 hours. Three dimensional response graphs were presented to visualize the effect of independent variables on the chosen response. Thus, Eudragit S100 microspheres can be successfully prepared for oral delivery of enzymes with desirable characters in terms of maximum loading and diffusion release pattern.
Starting Page	289
Ending Page	297
Page Count	9
File Format	PDF
Journal	AAPS PharmSciTech
Volume Number	8
Issue Number	4
e-ISSN	15309932
Language	English
Publisher	Springer-Verlag
Publisher Date	2007-01-01
Publisher Institution	American Association of Pharmaceutical Scientists
Publisher Place	New York
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Enzyme delivery factorial design Tween 80 microspheres 3D response graphs Pharmacology/Toxicology Biotechnology Biochemistry Pharmacy
Content Type	Text
Resource Type	Article

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