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Author Latha, M. S. ♦ Lal, A. V. ♦ Kumari, T. V. ♦ Sreekumar, R. ♦ Jayakrishnan, A.
Source Sree Chitra Tirunal Institute for Medical Sciences & Technology
Content type Text
Publisher Contraception
File Format PDF
Language English
Subject Domain (in DDC) Technology ♦ Medicine & health ♦ Pharmacology and therapeutics
Subject Domain (in MeSH) Therapeutics ♦ Investigative Techniques ♦ Analytical, Diagnostic and Therapeutic Techniques and Equipment
Subject Keyword Drug Delivery
Abstract Microspheres of bovine milk protein casein loaded with progesterone were fabricated by glutaraldehyde cross-linking of an aqueous alkaline solution of the protein dispersed in a hexane and dichloromethane non-aqueous dispersion medium with an aliphatic polyurethane as the stabilizer. Microspheres were characterized for their surface morphology and internal structure using scanning electron microscopy. In vitro release studies in phosphate buffer at 37 degrees C demonstrated that the rate of release of the steroid from the microsphere matrix was a function of cross-linking density, particle size, and drug payload. Microsphere formulations released 50% to 60% of the incorporated steroid in about 30 days and, thereafter, attained a steady state. in the presence of a protein-digesting enzyme such as protease, complete release of the steroid was observed in about 4 days in vitro into phosphate buffer. Intramuscular injection of progesterone-loaded microspheres into rabbits showed a plasma concentration of 1 to 2 ng/mL up to 5 months without any significant burst effect, whereas the powdered steroid administered in saline demonstrated a large burst effect peaking over 20 ng/mL, and the plasma concentration was not sustained beyond 4 days. Data obtained suggest that casein microspheres would be promising as a biodegradable drug carrier for sustained delivery of steroids. (C) 2000 Elsevier Science Inc. All rights reserved.
Education Level UG and PG
Learning Resource Type Article
Educational Framework Medical Council of India (MCI)
Journal CONTRACEPTION
Volume Number 61
Issue Number 5
Page Count 6
Starting Page 329
Ending Page 334