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Title: Development of delayed-release proliposomes tablets for oral protein drug delivery
Authors: Charintra Tantisripreecha
Montree Jaturanpinyo
Busaba Panyarachun
Narong Sarisuta
Mahidol University
Faculty of Medicine, Thammasat University
Keywords: Chemistry;Pharmacology, Toxicology and Pharmaceutics
Issue Date: 1-Jun-2012
Citation: Drug Development and Industrial Pharmacy. Vol.38, No.6 (2012), 718-727
Abstract: Context: One among many attempts to improve oral protein drug delivery was utilizing the colloidal drug carriers particularly liposomes. Objective: The purpose was to develop proliposomes of bovine serum albumin (BSA) in the form of granules and delayed-release tablets by using simple tablet manufacturing process. Materials and methods: BSA proliposomes granules were prepared by spraying 7:3 (w/w) lecithin:cholesterol solution mixture onto BSA-mannitol granules rotating in a glass coating pan. BSA proliposomes granules were directly compressed into tablets and subsequently coated with Eudragit® L100 film. The physical properties and stability in gastrointestinal fluids of delayed-release BSA proliposomes tablets as well as reconstituted liposomes were assessed. Results: The BSA proliposomes tablets disintegrated readily and the obtained reconstituted BSA liposomes exhibited multilamellar vesicles, the size and entrapment efficiency of which were around 23 m and 1014%, respectively. The delayed-release BSA proliposomes tablets were found to be relatively stable in United States Pharmacopoeia (USP) simulated gastric and intestinal fluids. Increase in amount of BSA in granules resulted in the increase in entrapment efficiency and loading capacity. Discussion: The Fourier transform infrared spectroscopy (FTIR) results indicated increase in α-helix structure of BSA entrapped in liposomes. 31 P phosphorous nuclear magnetic resonance spectroscopy ( 31 P-NMR) spectrum indicated interaction between BSA molecules and phosphoric acid polar groups of bilayers membrane. Conclusion: The delayed-release BSA proliposomes tablets developed could completely be reconstituted into liposomes with sufficient resistance to the hostile environment in gastrointestinal tract. © 2012 Informa Healthcare USA, Inc.
ISSN: 15205762
Appears in Collections:Scopus 2011-2015

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