Abstract
Purpose: To formulate piroxicam-loaded lipospheres and evaluate their in vitro and in vivo properties.Method: Piroxicam-loaded lipospheres were prepared by hot homogenization technique using dika wax and Phospholipon® 90G (1:1, 1:2 and 2:1) as the lipid matrix. Characterisation, based on particle sizeand morphology, pH, drug content and encapsulation efficiency, were carried out on the lipospheres. In vitro release was evaluated in simulated intestinal fluid (pH 7.5). Anti-inflammatory and ulcerogenic properties of the piroxicam-loaded lipospheres were studied using healthy, adult Wistar rats.Result: Photomicrographs revealed spherical particles in the range of 1.66 – 3.56 ìm. The results also indicated that lipospheres formulated with lipid matrix 1:1 and containing 0.25 % piroxicam had the highest encapsulation efficiency of 84 %. In vitro release data showed that lipospheres formulated with lipid matrix having higher concentration of dika wax exhibited the fastest drug release of drug with maximum release time between 60 - 70 min. The lipospheres exhibited good anti-inflammatoryproperties with 58.6 % oedema inhibition at 5 h. Piroxicam-loaded liposheres had an ulcer index of zero while, the reference (plain piroxicam) had an ulcer index of 15.00 ± 1.23 (p < 0.05).Conclusion: Piroxicam lipospheres formulated with a mixture of dika wax and phospholipid exhibited good in vitro and in vivo properties.Keywords: Dika wax, Lipospheres, Piroxicam, Phospholipid, Ulcerogenicity, Anti-inflammatory
Highlights
The rapid growth in the use of lipid-based drug delivery systems is primarily due to the diversity and versatility of pharmaceutical grade lipid excipients and their compatibility with liquid, semi-solid and solid drugs [1]
The combination of a solid inner core and a phospholipid exterior confers several advantages on the lipospheres compared with conventional microspheres, such as high dispersibility in an aqueous medium, and a release rate for the entrapped substance that is controlled by phospholipid coating and carrier [6,7]
The lipospheres formulated with higher content of phospholipid (2:1) in the lipid matrix, i.e., batches C1 to C3 greater prolonged drug release behaviour with maximum drug release at 120 min
Summary
The rapid growth in the use of lipid-based drug delivery systems is primarily due to the diversity and versatility of pharmaceutical grade lipid excipients and their compatibility with liquid, semi-solid and solid drugs [1]. The increasing availability of lipidic excipients with specific characteristics offer flexibility of application with respect to improving the bioavailability of poorly water soluble drugs and manipulating their release profile [2]. Dika wax is an edible vegetable fat derived from the kernel of Irvingia gabonensis Var excelcia [3,4]. It is a completely biodegradable physiological lipid, and like other lipid excipients, it has a GRAS (generally regarded as safe) status. The danger of use of synthetic polymer matrix forming materials which may be associated with detrimental effects on incorporated drug during manufacturing of formulations or during the erosion of the polymers after application is completely avoided [5]. The combination of a solid inner core and a phospholipid exterior confers several advantages on the lipospheres compared with conventional microspheres, such as high dispersibility in an aqueous medium, and a release rate for the entrapped substance that is controlled by phospholipid coating and carrier [6,7]
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