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Synthesis and evaluation of novel polyester-ibuprofen conjugates for modified drug release.
Drug Dev Ind Pharm 2008; 34(8):877-84DD

Abstract

Ibuprofen was conjugated at different levels to a novel polyester, poly(glycerol-adipate-co-omega-pentadecalactone) (PGA-co-PL), via an ester linkage to form a prodrug. The conjugates were characterized by differential scanning calorimetry (DSC), nuclear magnetic resonance (NMR), infrared (IR), gel permeation chromatography (GPC), ultraviolet (UV), and high-performance liquid chromatography (HPLC). The conjugates had a molecular weight between 18 and 24 kDa, and there was a suppression of the free hydroxyl groups within the conjugated polymer. DSC scans showed a lowering of the melting point (T(m)) when compared with the polyester alone and a difference in the number and area of T(m) peaks. Drug release studies showed an initial burst release (13-18%) followed thereafter by very slow release (maximum 35% after 18 days). Continuous work may produce ester-linked conjugates that are sufficiently labile to allow for complete release of ibuprofen over the time period studied.

Authors+Show Affiliations

School of Pharmacy, The Robert Gordon University, Aberdeen, Scotland.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

18622877

Citation

Thompson, C J., et al. "Synthesis and Evaluation of Novel Polyester-ibuprofen Conjugates for Modified Drug Release." Drug Development and Industrial Pharmacy, vol. 34, no. 8, 2008, pp. 877-84.
Thompson CJ, Hansford D, Munday DL, et al. Synthesis and evaluation of novel polyester-ibuprofen conjugates for modified drug release. Drug Dev Ind Pharm. 2008;34(8):877-84.
Thompson, C. J., Hansford, D., Munday, D. L., Higgins, S., Rostron, C., & Hutcheon, G. A. (2008). Synthesis and evaluation of novel polyester-ibuprofen conjugates for modified drug release. Drug Development and Industrial Pharmacy, 34(8), pp. 877-84. doi:10.1080/03639040801929075.
Thompson CJ, et al. Synthesis and Evaluation of Novel Polyester-ibuprofen Conjugates for Modified Drug Release. Drug Dev Ind Pharm. 2008;34(8):877-84. PubMed PMID: 18622877.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Synthesis and evaluation of novel polyester-ibuprofen conjugates for modified drug release. AU - Thompson,C J, AU - Hansford,D, AU - Munday,D L, AU - Higgins,S, AU - Rostron,C, AU - Hutcheon,G A, PY - 2008/7/16/pubmed PY - 2008/9/19/medline PY - 2008/7/16/entrez SP - 877 EP - 84 JF - Drug development and industrial pharmacy JO - Drug Dev Ind Pharm VL - 34 IS - 8 N2 - Ibuprofen was conjugated at different levels to a novel polyester, poly(glycerol-adipate-co-omega-pentadecalactone) (PGA-co-PL), via an ester linkage to form a prodrug. The conjugates were characterized by differential scanning calorimetry (DSC), nuclear magnetic resonance (NMR), infrared (IR), gel permeation chromatography (GPC), ultraviolet (UV), and high-performance liquid chromatography (HPLC). The conjugates had a molecular weight between 18 and 24 kDa, and there was a suppression of the free hydroxyl groups within the conjugated polymer. DSC scans showed a lowering of the melting point (T(m)) when compared with the polyester alone and a difference in the number and area of T(m) peaks. Drug release studies showed an initial burst release (13-18%) followed thereafter by very slow release (maximum 35% after 18 days). Continuous work may produce ester-linked conjugates that are sufficiently labile to allow for complete release of ibuprofen over the time period studied. SN - 1520-5762 UR - https://www.unboundmedicine.com/medline/citation/18622877/Synthesis_and_evaluation_of_novel_polyester_ibuprofen_conjugates_for_modified_drug_release_ L2 - http://www.tandfonline.com/doi/full/10.1080/03639040801929075 DB - PRIME DP - Unbound Medicine ER -