Development and Characterisation of Natamycin Mini-Matrices Prepared by Hot-Melt Extrusion for Vaginal Delivery
- 1 Department of Pharmaceutical Technology, Faculty of Pharmacy, Izmir Katip Celebi University, Izmir, Turkey
- 2 Department of Pharmaceutical Technology, Faculty of Pharmacy, Ege University, Izmir, Turkey
Abstract
In this study, bioadhesive mini-matrices of natamycin were prepared for vaginal application by hot-melt extrusion. In addition, melt viscosity measurements, thermogravimetric analysis, in vitro drug release studies and in vitro mucoadhesion test were performed. High molecular weight grades of KlucelTM hydroxypropylcellulose were used as a thermoplastic polymer. TEC and PEG 400 were chosen as plasticizer. According to the obtained results of melt viscosity measurements, the maximum torque of extrudates prepared using PEG 400 increased with increasing drug loading. The thermo-gravimetric analyses showed that natamycin is stable up to 198℃ and this result gives the opportunity to hot melt extrussion process at 90℃. In vitro drug release results showed that the release was extended up to 72 hours and drug release rate increased with increasing drug loading. In respect to the in vitro mucoadhesion test results, the values of work of mucoadhesion were found high as 771,977 mN.mm, 753,199 mN.mm, 686,356 mN.mm for the prepared hot melt extruded mini-matrices. Our results showed that the developed formulations were found worthy of further studies.
- Johal, H.S., Garg, T., Rath, G. and Goyal, A.K. (2016). Advanced Topical Drug Delivery System for the Management of Vaginal Candidiasis. Drug Delivery, 23, 550-563. https://doi.org/10.3109/10717544.2014.928760
- Nyirjesy, P. (2008) Vulvovaginal Candidiasis and Bacterial Vaginosis. Infectious Disease Clinics of North America, 22, 637-652. https://doi.org/10.1016/j.idc.2008.05.002
- Rosalinde, H. and Louvois, J.D. (1979) Candida Vaginitis. Postgraduate Medical Journal, 55, 645-647. https://doi.org/10.1136/pgmj.55.647.645
- Jack, D.S., Wiesenfelt, H.C., Martens, M., Danna, P., Hooton, T.M., Rompalo, A., Sperling, M., Livengood III, C., Horowitz, B., Thron, J.V., Edwards, L., Panzer, H. and Chu, T.C. (2004) Maintenance Fluconazole Therapy for Recurrent Vulvovaginal Candidiasis. The New England Journal of Medicine, 351, 876-883. https://doi.org/10.1056/NEJMoa033114
- Kalavathy, C.M., Parmar, P., Kal-iamurthy, J., Philip, V.R., Ramalingam, M.D.K., Jesudasan, C.A.N. and Thomas, P.A. (2005) Comparison of Topical Itraconazole 1% with Topical Natamycin 5% for the Treatment of Filamentous Fungal Keratitis. Clinical Sciences, 24, 449-452. https://doi.org/10.1097/01.ico.0000151539.92865.3e
- Fucinos, C., Guerra, N.P., Teijon, J.M., Pastrana, L.M., and Katime, I. (2012) Use of poly(N-isopropylacrylamide) Nanohydrogels for the Controlled Release of Pimaricin in Active Packaging. Journal of Food Science, 77, 21-28. https://doi.org/10.1111/j.1750-3841.2012.02781.x
- Ozguney, I., Shuwisitkul, D. and Bodmeier, R. (2009) Development and Characterization of Extended Release Kollidon SR Mini-Matrices Prepared by Hot-Melt Extrusion. European Journal of Pharmaceutics and Biopharmaceutics, 73, 140-145. https://doi.org/10.1016/j.ejpb.2009.04.006
- Zhu, Y., Navnit, H.S., Malick, A.W., Infeld, M.H. and McGinity, J.W. (2006) Controlled Release of a Poorly Water-Soluble Drug from Hot-Melt Extrudates Containing Acrylic Polymers. Drug Development and Industrial Pharmacy, 32, 569-583. https://doi.org/10.1080/03639040500528996
- Alexander, N.J., Baker, E., Kaptein, M., Karck, U., Miller, L. and Zampaglione, E. (2004) Why Consider Vaginal Drug Administration? Fertility and Sterility, 82, 1-12. https://doi.org/10.1016/j.fertnstert.2004.01.025
- Vermani, K. and Garg, S. (2000) The Scope and Potential of Vaginal Drug Delivery. PSTT, 3, 359-364. https://doi.org/10.1016/S1461-5347(00)00296-0
- Duchêne, D. and Ponchel, G. (1992) Principle and Investigation of the Bioadhesion Mechanism of Solid Dosage Forms. Biomaterials, 13, 709-714. https://doi.org/10.1016/0142-9612(92)90132-8