Biodegradable injectable implant systems for sustained delivery using poly (lactide-co-glycolide) copolymers

M. Madhu, L. Shaila, B.J. Anwar

Research output: Contribution to journalArticle

12 Citations (Scopus)

Abstract

Poly (lactide-co-glycolide) (PLG) is one of the most widely used biodegradable synthetic polymer for sustained release formulations. In the present work, in situ gel formulation has been developed using poly (lactide-co-glycolide) to deliver an antidiabetic drug- rosiglitazone, that can be given by subcutaneous route. The effect of different vehicles (N-methyl-2-pyrrolidone, triacetin), polymer concentration and comonomer ratios such as (65:35, 75:25, 85:15) in the polymer on the release of drug from the formulation were studied. The initial burst effect was substantially reduced when the PLG concentration was increased. Out of different comonomer ratios of PLG, the ratio 85:15 showed more sustained release with comparatively less burst effect. The formulations containing triacetin as the solvent showed controlled release of the drug with least burst effect. Good sustained and prolonged release of the drug coupled with biocompatibility characteristics make injectable in situ gel forming implant systems of PLG, a prospective implantable controlled release dosage form to deliver the drug in the therapy of diabetes.
Original languageEnglish
Pages (from-to)103-107
Number of pages5
JournalInternational Journal of Pharmacy and Pharmaceutical Sciences
Volume1
Issue numberSUPPL. 1
Publication statusPublished - 2009

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Absorbable Implants
Polyglactin 910
Triacetin
Polymers
rosiglitazone
Injections
Gels
Drug Compounding
Dosage Forms
Hypoglycemic Agents
Drug Therapy
Drug Liberation

Cite this

@article{905dc5e0775447e5b42fdfa54881607b,
title = "Biodegradable injectable implant systems for sustained delivery using poly (lactide-co-glycolide) copolymers",
abstract = "Poly (lactide-co-glycolide) (PLG) is one of the most widely used biodegradable synthetic polymer for sustained release formulations. In the present work, in situ gel formulation has been developed using poly (lactide-co-glycolide) to deliver an antidiabetic drug- rosiglitazone, that can be given by subcutaneous route. The effect of different vehicles (N-methyl-2-pyrrolidone, triacetin), polymer concentration and comonomer ratios such as (65:35, 75:25, 85:15) in the polymer on the release of drug from the formulation were studied. The initial burst effect was substantially reduced when the PLG concentration was increased. Out of different comonomer ratios of PLG, the ratio 85:15 showed more sustained release with comparatively less burst effect. The formulations containing triacetin as the solvent showed controlled release of the drug with least burst effect. Good sustained and prolonged release of the drug coupled with biocompatibility characteristics make injectable in situ gel forming implant systems of PLG, a prospective implantable controlled release dosage form to deliver the drug in the therapy of diabetes.",
author = "M. Madhu and L. Shaila and B.J. Anwar",
note = "Cited By :9 Export Date: 10 November 2017 Correspondence Address: Shaila, L.; Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal-576 104, India; email: s.lewis@manipal.edu Chemicals/CAS: 1 methyl 2 pyrrolidinone, 872-50-4; polyglactin, 26780-50-7, 34346-01-5; rosiglitazone, 122320-73-4, 155141-29-0; triacetin, 102-76-1 Manufacturers: Aristo Pharmaceuticals, India; birmingham, United Kingdom; Sigma, United States References: Zhidong, L., Jiawei, L., Shufang, N., Hui, L., Weisan, P., Study of an alginate/HPMC-based in situ gelling ophthalmic delivery system for gatifloxacin (2006) Int. J. Pharm, 315, pp. 12-16; Peppas, N.A., Langer, A., New challenges in biomaterials (1994) Science, pp. 263-1715; Lange, R., New method of drug delivery (1981) Science, pp. 240-1533; Hatefi, A., Amsden, B., Biodegradable injectable insitu forming drug delivery systems (2002) J.Control Release, 80, p. 9; Dunn, R.L., English, J.P., Cowsar, D.R., Vanderbelt, D.P., (1990), US patent 4938763. 3 July; Boehm, Garth, Dundon Josephine. Rosiglitazone formulations. WO/2 005/065654; Krentz, A.J., Bailey, C.J., Oral antidiabetic agents: Current role in type 2 diabetes mellitus (2005) Drugs, 65, pp. 385-411; Shah, N.H., Railkar, A.S., Chen, F.C., Tarantino, R., Kumar, S., Murjani, M., Palmer, D., Malick, A.W., A biodegradable injectable implant for delivering micro and macro molecules using poly (lactic-co-glycolic) acid (PLGA) copolymers (1993) J. Control Release, pp. 27-139; Chandrashekar, G., Udupa, N., Biodegradable injectable implants for long term drug delivery using poly (lacticco-glycolic) acid (PLGA) copolymers (1998) J. Pharm.Pharmacol, 48, p. 669; Huang, X., Brazel, C.S., On the importance and mechanism of burst release in matrix controlled drug delivery systems (2001) J. Control Release, 73, p. 121; Lambert, W.J., Peck, K.D., Development of an in situ forming biodegradable poly lactide co glycolide system for the controled release of proteins (1995) J. Control Release, 33, p. 189; Shively, M.L., Benett, A.T., Coons, B.A., Renner, W.D., Southard, J.L., Physicochemical characterization of a polymeric injectable implant delivery system (1995) J. Control Release, pp. 33-237",
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pages = "103--107",
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issn = "0975-1491",
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Biodegradable injectable implant systems for sustained delivery using poly (lactide-co-glycolide) copolymers. / Madhu, M.; Shaila, L.; Anwar, B.J.

In: International Journal of Pharmacy and Pharmaceutical Sciences, Vol. 1, No. SUPPL. 1, 2009, p. 103-107.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Biodegradable injectable implant systems for sustained delivery using poly (lactide-co-glycolide) copolymers

AU - Madhu, M.

AU - Shaila, L.

AU - Anwar, B.J.

N1 - Cited By :9 Export Date: 10 November 2017 Correspondence Address: Shaila, L.; Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal-576 104, India; email: s.lewis@manipal.edu Chemicals/CAS: 1 methyl 2 pyrrolidinone, 872-50-4; polyglactin, 26780-50-7, 34346-01-5; rosiglitazone, 122320-73-4, 155141-29-0; triacetin, 102-76-1 Manufacturers: Aristo Pharmaceuticals, India; birmingham, United Kingdom; Sigma, United States References: Zhidong, L., Jiawei, L., Shufang, N., Hui, L., Weisan, P., Study of an alginate/HPMC-based in situ gelling ophthalmic delivery system for gatifloxacin (2006) Int. J. Pharm, 315, pp. 12-16; Peppas, N.A., Langer, A., New challenges in biomaterials (1994) Science, pp. 263-1715; Lange, R., New method of drug delivery (1981) Science, pp. 240-1533; Hatefi, A., Amsden, B., Biodegradable injectable insitu forming drug delivery systems (2002) J.Control Release, 80, p. 9; Dunn, R.L., English, J.P., Cowsar, D.R., Vanderbelt, D.P., (1990), US patent 4938763. 3 July; Boehm, Garth, Dundon Josephine. Rosiglitazone formulations. WO/2 005/065654; Krentz, A.J., Bailey, C.J., Oral antidiabetic agents: Current role in type 2 diabetes mellitus (2005) Drugs, 65, pp. 385-411; Shah, N.H., Railkar, A.S., Chen, F.C., Tarantino, R., Kumar, S., Murjani, M., Palmer, D., Malick, A.W., A biodegradable injectable implant for delivering micro and macro molecules using poly (lactic-co-glycolic) acid (PLGA) copolymers (1993) J. Control Release, pp. 27-139; Chandrashekar, G., Udupa, N., Biodegradable injectable implants for long term drug delivery using poly (lacticco-glycolic) acid (PLGA) copolymers (1998) J. Pharm.Pharmacol, 48, p. 669; Huang, X., Brazel, C.S., On the importance and mechanism of burst release in matrix controlled drug delivery systems (2001) J. Control Release, 73, p. 121; Lambert, W.J., Peck, K.D., Development of an in situ forming biodegradable poly lactide co glycolide system for the controled release of proteins (1995) J. Control Release, 33, p. 189; Shively, M.L., Benett, A.T., Coons, B.A., Renner, W.D., Southard, J.L., Physicochemical characterization of a polymeric injectable implant delivery system (1995) J. Control Release, pp. 33-237

PY - 2009

Y1 - 2009

N2 - Poly (lactide-co-glycolide) (PLG) is one of the most widely used biodegradable synthetic polymer for sustained release formulations. In the present work, in situ gel formulation has been developed using poly (lactide-co-glycolide) to deliver an antidiabetic drug- rosiglitazone, that can be given by subcutaneous route. The effect of different vehicles (N-methyl-2-pyrrolidone, triacetin), polymer concentration and comonomer ratios such as (65:35, 75:25, 85:15) in the polymer on the release of drug from the formulation were studied. The initial burst effect was substantially reduced when the PLG concentration was increased. Out of different comonomer ratios of PLG, the ratio 85:15 showed more sustained release with comparatively less burst effect. The formulations containing triacetin as the solvent showed controlled release of the drug with least burst effect. Good sustained and prolonged release of the drug coupled with biocompatibility characteristics make injectable in situ gel forming implant systems of PLG, a prospective implantable controlled release dosage form to deliver the drug in the therapy of diabetes.

AB - Poly (lactide-co-glycolide) (PLG) is one of the most widely used biodegradable synthetic polymer for sustained release formulations. In the present work, in situ gel formulation has been developed using poly (lactide-co-glycolide) to deliver an antidiabetic drug- rosiglitazone, that can be given by subcutaneous route. The effect of different vehicles (N-methyl-2-pyrrolidone, triacetin), polymer concentration and comonomer ratios such as (65:35, 75:25, 85:15) in the polymer on the release of drug from the formulation were studied. The initial burst effect was substantially reduced when the PLG concentration was increased. Out of different comonomer ratios of PLG, the ratio 85:15 showed more sustained release with comparatively less burst effect. The formulations containing triacetin as the solvent showed controlled release of the drug with least burst effect. Good sustained and prolonged release of the drug coupled with biocompatibility characteristics make injectable in situ gel forming implant systems of PLG, a prospective implantable controlled release dosage form to deliver the drug in the therapy of diabetes.

M3 - Article

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SP - 103

EP - 107

JO - International Journal of Pharmacy and Pharmaceutical Sciences

JF - International Journal of Pharmacy and Pharmaceutical Sciences

SN - 0975-1491

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ER -