PREPARATION AND CHARACTERIZATION OF STAVUDINE ENTRAPPED LIPOSPHERES
Lipospheres of stavudine were prepared by melt dispersion technique using trimyristin, tripalmitin and triastearin, stearic acid, Compritol® 888 ATO and Precirol® ATO 5 as lipid matrix in the various drug-lipid ratios. Drug entrapped free flowing solid lipospheres of triglycerides and glyceryl behenate were characterized for surface morphology, particle size distribution, encapsulation efficiency, and in vitrorelease behavior. The effect of drug lipid ratio, the surfactant used, concentration of stabilizer, and stirring speed were identified as the key variables affecting the formation of discrete spherical lipospheres and sustained drug release rate. The lipospheres production conditions were optimized by using 2% w/w sodium cholate and 1% Plural oleic as a stabilizer. The concentration of lipid used had pronounced effect on particle size of the lipospheres. The incorporation efficiency was found to be in range of 30 to 50%. Increase in concentration of surfactant and stirring speed produced fine spherical, smooth, and round lipospheres. All the prepared lipospheres exhibited slow release profiles dictating the Higuchi mode of release.Key words: Lipospheres, stavudine, lipid matrix, hydrophilic surfactant, drug release
Amselem, S., Alving, C.R.,Domb, A.J., Lipospheres for vaccine delivery. Drugs Pharm. Sci., 1996, 77: 149–168.
Alonso, M.J., Nanomedicines for overcoming biological barriers. Biomed. Pharmacother., 2004, 58(3): 168-172.
Attama, A.A., Okafor, C.E., Builders, P.F.,Okorie, O., Formulation and in vitro evaluation of a PEGylated microscopic lipospheres delivery system for ceftriaxone sodium. Drug Deliv., 2009, 16(8): 448-457.
Bekerman, T., Golenser, J.,Domb, A., Cyclosporin nanoparticulate lipospheres for oral administration. J. Pharm. Sci., 2004, 93(5): 1264-1270.
Cortesi, R., Esposjto, E., Luca, G.,Nastruzzi, C., Production of lipospheres as carriers for bioactive compounds. Biomaterials, 2002, 23(11): 2283-2294.
Elgart, A., Cherniakov, I., Aldouby, Y., Domb, A.J.,Hoffman, A., Lipospheres and pronano lipospheres for delivery of poorly water soluble compounds. Chem. Phys. Lipids, 2012, 165(4): 438-453.
El-Gibaly, I.,Abdel-Ghaffar, S.K., Effect of hexacosanol on the characteristics of novel sustained-release allopurinol solid lipospheres (SLS): factorial design application and product evaluation. Int. J. Pharm., 2005, 294(1-2): 33-51.
Hersh, E.V., Maniar, M., Green, M.,Cooper, S.A., Anesthetic activity of the lipospheres bupivacaine delivery system in the rat. Anesth. Prog., 1992, 39(6): 197-200.
Khopade, A.J.,Jain, N.K., Long-circulating lipospheres targeted to the inflammed tissue. Die Pharmazie, 1997, 52(2): 165-166.
Nasr, M., Mansour, S., Mortada, N.D.,El Shamy, A.A., Lipospheres as carriers for topical delivery of aceclofenac: preparation, characterization and in vivo evaluation. AAPS PharmSciTech, 2008, 9(1): 154-162.
Pandit, S.S.,Patil, A.T., Formulation and in vitro evaluation of buoyant controlled release lercanidipine lipospheres. J. Microencapsul., 2009, 26(7): 635-641.
Shivakumar, H.N., Patel, P.B., Desai, B.G., Ashok, P.,Arulmozhi, S., Design and statistical optimization of glipizide loaded lipospheres using response surface methodology. Acta pharmaceutica, 2007, 57(3): 269-285.
Sznitowska, M., Janicki, S., Gajewska, M.,Kulik, M., Investigation of diazepam lipospheres based on Witepsol and lecithin intended for oral or rectal delivery. Acta Pol. Pharm., 2000, 57(1): 61-64.
Takenaga, M., 20, 209, 1996] Application of lipid microspheres for the treatment of cancer. Adv. Drug Del. Rev., 1996, 20: 209-219.
Toongsuwan, S., Li, L.C., Erickson, B.K.,Chang, H.C., Formulation and characterization of bupivacaine lipospheres. Int. J. Pharm., 2004, 280(1-2): 57-65.
Tursilli, R., Casolari, A., Iannuccelli, V.,Scalia, S., Enhancement of melatonin photostability by encapsulation in lipospheres. J. Pharm. Biomed. Anal., 2006, 40(4): 910-914.
Obaru, K.,Mitsuya, H., Anti-HIV drugs and drug delivery system. Nihon Rinsho, 1998, 56(3): 769-775.
Unger, E.C., McCreery, T.P., Sweitzer, R.H., Caldwell, V.E.,Wu, Y., Acoustically active lipospheres containing paclitaxel: a new therapeutic ultrasound contrast agent. Invest. Radiol., 1998, 33(12): 886-892.
Vyas, S.P., Singh, R.,Dimitrijevic, D., Development and characterization of nifedipine lipospheres. Die Pharmazie, 1997, 52(5): 403-404.
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