Mucoadhesive microspheres based formulation development of ziprasidone hydrochloride for nasal delivery
The purpose of research work was to develop and optimize mucoadhesive microspheres of Ziprasidone hydrochloride for nasal delivery with the aim to enhance the residence time and improve therapeutic efficacy. Mucoadhesive drug delivery systems are those that provide intimate contact of the drug with the mucosa for an extended period of time. In our present work, mucoadhesive chitosan microspheres were prepared by emulsification method using liquid paraffin as external phase. Ten different formulations were developed. Results show that as the concentration of polymer increases it affects the particle size, production yield, encapsulation efficiency, swelling index, in-vitro mucoadhesion and in-vitro drug release of mucoadhesive microspheres. The in vitro mucoadhesion of microspheres was investigated using freshly isolated goat nasal mucosa. The mucoadhesion for M0, M1, M2, and M9 was tested. The mucoadhesion property was satisfactory. The M2 exhibited lowest mucoadhesion of 68.9%, and M0 displayed highest mucoadhesion of 87.5%. The In Vitro release studies it revealed that 84.1% of drug release from formulation M1 at 7hrs. The 50% of the drug was released from the formulation M2 and 70.67% from formulation M9.This formulations were further used for SEM for particles size analysis, mucoadhesion test and in-vitro drug release. The In-vitro % drug release data suggest that the maximum and sustained drug release was obtained for formulation M1.The present study showed that Ziprasidone hydrochloride chitosan microspheres can deliver intanasally which can improve the therapeutic outcome for the Epileptic seizure.
Keywords: Ziprasidone hydrochloride, Mucoadhesive microspheres, Nasal drug delivery, Drug Entrapment efficiency.
2. Kamath KR, Park K, Sugbrick J, Boylen JC. Encyclopedia of Pharmaceutical Technology. New York: Marcel Dekker, 1994.
3. Jimen J, Castllanos MR, Zia H, Rhodes CT. Mucoadhesive drug delivery systems. Drug Dev Ind Pharm 1994; 19:143-154.
4. Illum L. Chitosan and its use as a pharmaceutical excipients. Pharm Res 1998; 15:1326-1331.
5. Takeuchi H, Yamamoto H, Niwa T, Hino T, Kawashima Y. Mucoadhesion of polymer coated liposomes to rat intestine in vitro. Chem Pharm Bull 1994; 42:1954-1960.
6. Chien YW, Su KSE, Chang SF. Nasal Systemic Drug Delivery. New York: Marcel Dekker. 1989.
7. El-Say KM, ElHelw AM, Ahmed OAA, Hosny KM, et al. Statistical optimization of controlled release microspheres containing cetirizine hydrochloride as a model for water soluble drugs. Informa Healthcare, 2014; 1-9.
8. Lehr CM, Bouwstra JA, Schacht EH, Junginger HE. In vitro evaluation of mucoadhesive properties of chitosan and some other natural polymers. Int J Pharm 1992; 78:43-8.
9. Singla AK, Chawla M. Chitosan, Some pharmaceutical and biological aspects-an update. J Pharm Pharmacol 2001; 53:1047-67.
10. Soane RJ, Frier M, Perkins AC, Jones NS, et al. Evaluation of the clearance characteristics of bioadhesive systems in humans. Int J Pharm 1999; 178:55-65.
11. Artursson P, Lindmark T, Davis SS, Illum L. Effect of chitosan on the permeability of monolayers of intestinal epithelial cells (Caco-2). Pharm Res 1994; 11:1358-61.
12. Sinha VR, Singla AK, Wadhawan S, Kaushik R, et al. Chitosan microspheres as a potential carrier for drugs. Int J Pharm 2004; 274:1-33.
13. Hafner A, Filipovic-Grcic J, Voinovich D, Jalsenjak I. Development and in vitro characterization of chitosanbased microspheres for nasal delivery of promethazine. Drug Dev Ind Pharm 2007; 33:427-36.
14. Asane GS, Nirmal SA, Rasal KB, Naik AA, et al. Polymers for mucoadhesive drug delivery system: A current status. Drug Dev Ind Pharm. 2008; 34:1246-66
15. Borse MP, Mulgund SV. UV Spectrophotometric estimation of ziprasidonein bulk and tablet dosage form. Der Pharm Lett, 2015; 7(5):272-275.
16. Varma MM, Begum R. Formulation, physicochemical evaluation, and dissolution studies of ziprasidonesolid dispersions. Int J Pharm Sci Nanotec, 2012; 5(3):56-59.
17. Kumar RT, Umamaheswari S. FTIR, FTR and UV-Vis analysis of carbamazepine. Res J Pharm Biol Chem, 2011; 2(4):78-84.
18. Pajander J, Rensonnet A, Øvergård M, Olsen MR, et al. Solid form change of Ziprasidoneduring hot melt processing. Thermochimica Acta 1995; 248:259-269.
19. Mitra A, Dey B. Chitosan microspheres in novel drug delivery systems. Indian J Pharm Sci. 2011; 73(4):355-366.
20. El-Hameed MDA, Kellaway IW. Preparation and in vitro characterisation of mucoadhesive polymeric microspheres as intra-nasal delivery systems. Eur J Pharm Biopharm 1997; 44:53-60.
21. Lamprecht A, Torres HR, Schäfer U, Lehr CM. Biodegradable microparticles as a two-drug controlled release formulation: a potential treatment of inflammatory bowel disease. J Contr Rel. 2000; 69:445-454.
22. Doddayya H, Srishailgouda SP, Reddy BT, Kumar P, et al. formulation and evaluation of brain-targeted nasal selegiline hydrochloride microspheres. Int J Pharm Biomed Res 2014; 20:123-156.
23. Gavini E, Hegge AB, Rassu G, Sanna V, et al. nasal administration of ziprasidoneusing chitosan microspheres: in vitro/in vivo studies. Int J Pharm.2006; 307:9-15.
24. Charulatha R, Rajan RK. Design and evaluation of Ziprasidone controlled release drug delivery system. Int J Pharm Tech Research, 2012; 2:23-45.
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