Prolonged release biodegradable vesicular carriers for rifampicin - Formulation and kinetics of release

M.P. Kamath, B.D. Shenoy, S.B. Tiwari, R. Karki, N. Udupa, M. Kotian

Research output: Contribution to journalArticle

13 Citations (Scopus)

Abstract

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.
Original languageEnglish
Pages (from-to)113-118
Number of pages6
JournalIndian Journal of Experimental Biology
Volume38
Issue number2
Publication statusPublished - 2000

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Rifampin
Liposomes
Pharmaceutical Preparations
Pharmacokinetics
Subcutaneous Injections
Drug Delivery Systems
Biological Availability
Half-Life
Lipids
Drug Liberation
In Vitro Techniques

Cite this

Kamath, M.P. ; Shenoy, B.D. ; Tiwari, S.B. ; Karki, R. ; Udupa, N. ; Kotian, M. / Prolonged release biodegradable vesicular carriers for rifampicin - Formulation and kinetics of release. In: Indian Journal of Experimental Biology. 2000 ; Vol. 38, No. 2. pp. 113-118.
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abstract = "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.",
author = "M.P. Kamath and B.D. Shenoy and S.B. Tiwari and R. Karki and N. Udupa and M. Kotian",
note = "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: info@mahe.ernet.in 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., Moran{\cc}ais, 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",
year = "2000",
language = "English",
volume = "38",
pages = "113--118",
journal = "Journal of scientific & industrial research. C. Biological sciences",
issn = "0019-5189",
publisher = "National Institute of Science Communication",
number = "2",

}

Prolonged release biodegradable vesicular carriers for rifampicin - Formulation and kinetics of release. / Kamath, M.P.; Shenoy, B.D.; Tiwari, S.B.; Karki, R.; Udupa, N.; Kotian, M.

In: Indian Journal of Experimental Biology, Vol. 38, No. 2, 2000, p. 113-118.

Research output: Contribution to journalArticle

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: info@mahe.ernet.in 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

VL - 38

SP - 113

EP - 118

JO - Journal of scientific & industrial research. C. Biological sciences

JF - Journal of scientific & industrial research. C. Biological sciences

SN - 0019-5189

IS - 2

ER -