Biocompatible dendrimer for the solubility enhancement and sustained release of piroxicam

Murugan, E ; Yogaraj, V ; Geetharani, D P

Abstract

Piroxicam (PRM) a nonsteroidal anti-inflammatory medication is an oxicam-class used orally to treat gout, arthritis, and other inflammatory diseases. However, its poor aqueous solubility and bioavailability has hampered further clinical applications in health industries. This work emphasize on development of four types of functionalised biocompatible dendrimer with generation 0 and 1and examine its solubility, drug release and antibacterial activity. The maximum solubility enhancement of PRM up to 48 folds has been achieved by PAMAM (G1)-CH3 at a concentration of 9.9×10-4 M. The in vitro release gets sustained up to 450 mins for releasing 90% of drug from PAMAM (G1)-COCH3 compared to its parent dendrimer which is 120 min. The anti-bacterial studies reflected that when dendrimers are used as drug carriers, the inherent property of drug is not disturbed, instead the activity has been increased. The activity interms of zone of inhibition results in 1.5-2.0 folds increase and it is more pronounced in the case of B. subtilis rather than E.coli. This observation indicates evidence that dendrimer and their derivatives are promising candidates for drug solubility enhancer and effective delivery of drugs with drastic reduction in side effect and improved efficiency.

Keyword(s)

Antibacterial activity; PAMAM dendrimer; Piroxicam (PRM); Solubility enhancement; Sustained release

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