Abstract
Purpose : To prepare and evaluate floating microspheres of curcumin for prolonged gastric residence time and increased drug bioavailability. Methods : Floating microsphere were prepared by emulsion solvent diffusion method, using hydroxylpropyl methylcellulose (HPMC), ethyl cellulose (EC), Eudragit S 100 polymer in varying ratios. Ethanol/dichloromethane blend was used as solvent in a ratio of 1:1. The floating microspheres were evaluated for flow properties, particle size, incorporation efficiency, as well as in-vitro floatability and drug release. The shape and surface morphology of the microspheres were characterised by optical and scanning electron microscopy. Result : The floating microspheres showed particle size, buoyancy, drug entrapment efficiency and yield in the ranges of 251 - 387 im, 74.6 - 90.6 %, and 72.6 - 83.5 %, and 45.5 - 82.0 %, respectively. Maximum drug release after 20 h was 47.1, 55.7, 69.4 and 81.3 % for formulations F1, F2, F3 and F4, respectively. Scanning electron micrographs indicate pores both on the surface and interior of the microspheres. Conclusion : The developed curcumin microsphere system is a promising floating drug delivery system for oral sustained administration of curcumin. Keywords : Gastro-retentive, Sustained release, Curcumin, Floating microspheres; Ethyl cellulose, Hydroxylpropyl methylcellulose, Eudragit
Highlights
In the past, herbal drugs did not attract researchers’ interest for the development of novel drug delivery systems due to difficulties in processing
With the advances in technology, new doors have been opened for the development of herbal drug delivery systems [1]
The floating microspheres were collected by decantation, washed thrice with n-hexane, dried overnight in an oven at 40 ± 2 oC, and stored in a desiccator containing calcium chloride as desiccant
Summary
Herbal drugs did not attract researchers’ interest for the development of novel drug delivery systems due to difficulties in processing (including standardization, extraction and identifycation). The floating microspheres beneficially alter the absorption of a drug, enhancing its bioavailability. They prolong dosing intervals which would allow development of once a day formulations and thereby increase patient compliance beyond the level of existing dosage forms by achieving control over gastric residence time [2,3]. Floating microspheres are gastroretentive drug delivery systems based on a non-effervescent approach. These microspheres are characteristically free-flowing powders having a size < 199 μm and remain buoyant over gastric contents for a prolonged period. The floating microspheres were collected by decantation, washed thrice with n-hexane, dried overnight in an oven at 40 ± 2 oC, and stored in a desiccator containing calcium chloride as desiccant
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