Journal
JOURNAL OF MICROENCAPSULATION
Volume 30, Issue 4, Pages 356-368Publisher
TAYLOR & FRANCIS LTD
DOI: 10.3109/02652048.2012.735263
Keywords
polyhydroxybutyrate; cellulose acetate phthalate; pharmacokinetics; pharmacodynamics; colon cancer; cytotoxicity
Funding
- Council of Scientific and Industrial Research, New Delhi, India [21/(0760)/09/EMR-II]
- India Council for Technical Education, New Delhi, India [AICTE. F. 1-51/RIFD/EF(13)/2011-12]
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Pharmacokinetics, biodistribution and antitumour activity of 5-fluorouracil (5-FU)-loaded polyhydroxybutyrate (PHB) and cellulose acetate phthalate (CAP) blend microspheres were investigated in chemically induced colorectal cancer in albino male Wistar rats and compared with pristine 5-FU given as a suspension. The microspheres were characterised for particle size, encapsulation efficiency, in vitro release and in vitro cytotoxicity on human HT-29 colon cancer cell line. Spherical particles with a mean size of 44 +/- 11 mm were obtained that showed sustained release of 5-FU. A high concentration of 5-FU was achieved in colonic tissues and significant reduction in tumour volume and multiplicity were observed in animals treated with 5-FU-loaded microspheres. The decreased levels of plasma albumin, creatinine, leucocytopenia and thrombocytopenia were observed in animals for 5-FU microspheres compared to the standard 5-FU formulation. The results suggest the extended release of 5-FU from the PHB-CAP blend microspheres in colonic region to enhance the antitumour efficacy.
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