In vitro characterization of methotrexate loaded poly(lactic-co-glycolic) acid microspheres and antitumor efficacy in Sarcoma-180 mice bearing tumor

U. V. Singh, N. Udupa

Research output: Contribution to journalArticle

22 Citations (Scopus)

Abstract

Methotrexate (MTX) loaded poly (lactic-co-glycolic) acid (PLGA) microspheres were prepared by emulsion solvent evaporation technique. The mean diameter of the microspheres was affected by the type of emulsion stabilizer, polymer concentration, aqueous and organic phase volume and stirring speed. The in vitro release was triphasic and was dependent on copolymer composition and molecular weight of the polymer. Antitumor efficacy in Sarcoma-180 tumor bearing mice exhibited increased volume doubling time (18 ± 2.7 days) compared to plain subcutaneous injection of methotrexate (8 ± 0.7 days). Preliminary pharmacokinetic studies following subcutaneous administration of MTX loaded PLGA microspheres illustrated the controlled release of the drug. The studies demonstrated the feasibility of employing PLGA as an effective carrier for antineoplastic drug like methotrexate.

Original languageEnglish
Pages (from-to)165-173
Number of pages9
JournalPharmaceutica Acta Helvetiae
Volume72
Issue number3
DOIs
Publication statusPublished - 06-1997

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Sarcoma 180
Microspheres
Methotrexate
Emulsions
Neoplasms
Polymers
Feasibility Studies
Subcutaneous Injections
Antineoplastic Agents
Pharmacokinetics
Molecular Weight
In Vitro Techniques
polylactic acid-polyglycolic acid copolymer

All Science Journal Classification (ASJC) codes

  • Molecular Medicine

Cite this

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title = "In vitro characterization of methotrexate loaded poly(lactic-co-glycolic) acid microspheres and antitumor efficacy in Sarcoma-180 mice bearing tumor",
abstract = "Methotrexate (MTX) loaded poly (lactic-co-glycolic) acid (PLGA) microspheres were prepared by emulsion solvent evaporation technique. The mean diameter of the microspheres was affected by the type of emulsion stabilizer, polymer concentration, aqueous and organic phase volume and stirring speed. The in vitro release was triphasic and was dependent on copolymer composition and molecular weight of the polymer. Antitumor efficacy in Sarcoma-180 tumor bearing mice exhibited increased volume doubling time (18 ± 2.7 days) compared to plain subcutaneous injection of methotrexate (8 ± 0.7 days). Preliminary pharmacokinetic studies following subcutaneous administration of MTX loaded PLGA microspheres illustrated the controlled release of the drug. The studies demonstrated the feasibility of employing PLGA as an effective carrier for antineoplastic drug like methotrexate.",
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AB - Methotrexate (MTX) loaded poly (lactic-co-glycolic) acid (PLGA) microspheres were prepared by emulsion solvent evaporation technique. The mean diameter of the microspheres was affected by the type of emulsion stabilizer, polymer concentration, aqueous and organic phase volume and stirring speed. The in vitro release was triphasic and was dependent on copolymer composition and molecular weight of the polymer. Antitumor efficacy in Sarcoma-180 tumor bearing mice exhibited increased volume doubling time (18 ± 2.7 days) compared to plain subcutaneous injection of methotrexate (8 ± 0.7 days). Preliminary pharmacokinetic studies following subcutaneous administration of MTX loaded PLGA microspheres illustrated the controlled release of the drug. The studies demonstrated the feasibility of employing PLGA as an effective carrier for antineoplastic drug like methotrexate.

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