TY - JOUR
T1 - Prolonged release biodegradable vesicular carriers for rifampicin - Formulation and kinetics of release
AU - Kamath, M.P.
AU - Shenoy, B.D.
AU - Tiwari, S.B.
AU - Karki, R.
AU - Udupa, N.
AU - Kotian, M.
N1 - Cited By :10
Export Date: 10 November 2017
CODEN: IJEBA
Correspondence Address: Udupa, N.; Department of Pharmaceutics, College of Pharmaceutical Sciences, Manipal 576 119, India; email: [email protected]
Chemicals/CAS: Antitubercular Agents; Delayed-Action Preparations; Drug Carriers; Liposomes; Rifampin, 13292-46-1
References: Gregoriadis, G., (1977) Nature, 265, p. 407; Sharma, A., Sharma, U.S., (1997) Int J Pharm, 154, p. 123; Uchegbu, I.F., Vyas, S.P., (1998) Int J Pharm, 172, p. 33; Jayakrishnan, A., Latha, M.S., (1997) Controlled and Novel Drug Delivery, p. 236. , edited by N K Jain, (CBS Publishers & Distributors, New Delhi); Brannon-Peppas, L., (1995) Int J Pharm, 116, p. 116; Gregoriadis, G., Florence, A.T., (1993) Drugs, 45, p. 15; Gregoriadis, G., (1995) Trends Biotechnol, 13, p. 527; Siler-Marinkovic, S., Mojovic, L., Davinic, V., Bugarski, B., (1997) Drug Dev Ind Pharm, 23, p. 483; Handjani-vila, R.M., Ribier, A., Rondot, B., Vanlerberghe, G., (1979) Int J Cosm Sci, 1, p. 303; Baillie, A.J., Florence, A.T., Hume, L.R., Muirhead, G.T., Rogerson, A., (1985) J Pharm Pharmacol, 37, p. 863; Azmin, M.N., Florence, A.T., Handjani-Vila, R.M., Stewert, J.F., Vanlerberghe, G., Whittaker, J.S., (1985) J Pharm Pharmacol, 37, p. 237; Ozer, A.Y., Hincal, A.A., Bouwstra, J.A., (1991) Eur J Pharm Biopharm, 37, p. 75; Vanlerberghe, G., Morançais, J.L., (1996) STP Pharma Sci, 6, p. 5; Zuidema, J., Kadir, F., Titulaer, H.A.C., Oussover, C., (1994) Int J Pharm, 105, p. 189; Shenoy, D.B., Singh, U.V., Udupa, N., Kumari, N., (1997) Indian J Pharmacol, 29, p. 233; Parthasarathi, G., Udupa, N., Uma Devi, P., Pillai, G.K., (1994) J Drug Targeting, 2, p. 173; D'Souza, S.A., Ray, J., Pandey, S., Udupa, N., (1997) J Pharm Pharmacol, 49, p. 145; Kamath, P.M., Shenoy, D.B., Karki, R., Udupa, N., Kotran, M., (1999) Indian Drugs, 36, p. 307; Rogerson, A., Cummings, J., Willmot, N., Florence, A.T., (1988) J Pharm Pharmacol, 40, p. 337; Hunter, C.A., Dolan, T.F., Coombs, G.H., Baillie, A.J., (1988) J Pharm Pharmacol, 40, p. 161; Harashima, H., Sakata, K., Funato, K., Kiwada, H., (1994) Pharm Res, 11, p. 402; Talsma, H., Crommelin, D.J.A., (1992) Pharm Technol, OCT, p. 96; Gabizon, A.A., Papahadjopoulos, D., (1988) Proc Natl Acad Sci USA, 85, p. 6949; Higuchi, T., (1963) J Pharm Sci, 52, p. 1145; Vyas, S.P., Goswami, S.K., Singh, R., (1995) Int J Pharm, 118, p. 23; Sharma, A., Straubinger, R.M., (1994) Pharm Res, 11, p. 889; Sheena, I.P., Singh, U.V., Aithal, K.S., Udupa, N., (1997) Pharm Sci, 3, p. 579; Raja Naresh, R.A., Udupa, N., (1996) STP Pharm Sci, 6, p. 61; Caselles, T.H., Villalain, J., Fernandez, G.J.C., (1990) J Pharm Sci, 42, p. 397; Lau, Y.Y., Hanson, G.D., Carel, B.J., (1996) J Chromatogr Biomed Appl, 676, p. 147; Gurevich, G.L., Berezovskaia, L.N., Manuilov, K.K., (1992) Antibiot Khimother, 37, p. 3; Sharma, A., Straubinger, N.L., Straubinger, R.M., (1993) Pharm Res, 11, p. 889
PY - 2000
Y1 - 2000
N2 - An attempt has been made to design suitable liposome and niosome-encapsulated drug delivery system for rifampicin and evaluated the same in vitro and in vivo. A modified lipid layer hydration method was employed to prepare these vesicular carriers. The formulated systems were characterized in vitro for size distribution analysis drug entrapment, drug release profiles and vesicular stability at different conditions of storage. In vivo drug kinetics was evaluated in normal, healthy albino rats for niosomal formulation upon subcutaneous injection and various pharmacokinetic parameters were determined. Niosomes and liposomes exhibited mean diameter of 9.73 and 11.87 μm with entrapment efficiencies of 30.5 and 34.2% respectively. Both the products exhibited sustained release characteristics in vitro with zero order drug release kinetics up to initial 10 hr. Stability evaluation indicated that both formulations were not significantly leaky over a period of one month. Niosomal formulation elevated plasma elimination half life and decreased elimination rate constants for rifampicin in vivo suggested that encapsulation retarded the removal of the drug from circulation compared to free drug due to slow drug release into systemic circulation. A five-fold increase in the area under plasma rifampicin concentration-time curve for niosomal rifampicin as compared to free drug indicated better bioavailability of encapsulated drug. It is evident from this study that niosomes and liposomes could be promising delivery systems for rifampicin with prolonged drug release profiles and reasonably good stability characteristics.
AB - An attempt has been made to design suitable liposome and niosome-encapsulated drug delivery system for rifampicin and evaluated the same in vitro and in vivo. A modified lipid layer hydration method was employed to prepare these vesicular carriers. The formulated systems were characterized in vitro for size distribution analysis drug entrapment, drug release profiles and vesicular stability at different conditions of storage. In vivo drug kinetics was evaluated in normal, healthy albino rats for niosomal formulation upon subcutaneous injection and various pharmacokinetic parameters were determined. Niosomes and liposomes exhibited mean diameter of 9.73 and 11.87 μm with entrapment efficiencies of 30.5 and 34.2% respectively. Both the products exhibited sustained release characteristics in vitro with zero order drug release kinetics up to initial 10 hr. Stability evaluation indicated that both formulations were not significantly leaky over a period of one month. Niosomal formulation elevated plasma elimination half life and decreased elimination rate constants for rifampicin in vivo suggested that encapsulation retarded the removal of the drug from circulation compared to free drug due to slow drug release into systemic circulation. A five-fold increase in the area under plasma rifampicin concentration-time curve for niosomal rifampicin as compared to free drug indicated better bioavailability of encapsulated drug. It is evident from this study that niosomes and liposomes could be promising delivery systems for rifampicin with prolonged drug release profiles and reasonably good stability characteristics.
M3 - Article
SN - 0019-5189
VL - 38
SP - 113
EP - 118
JO - Indian Journal of Experimental Biology
JF - Indian Journal of Experimental Biology
IS - 2
ER -