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Poly(glycerol adipate) - indomethacin drug conjugates - synthesis and in vitro characterization.
Int J Pharm 2017; 531(1):225-234IJ

Abstract

The linear biodegradable polyester poly(glycerol adipate) (PGA) was synthesized via enzymatic polycondensation using lipase B from Candida antarctica (CAL-B). Every monomer unit of PGA possesses a pendant hydroxyl group which is responsible for the hydrophilic character and moisture swelling. These OH groups were esterified to different degrees with the anti-inflammatory drug indomethacin in order to create a prodrug with a pH-sensitive linker for modified drug release. The structure of the conjugates was determined via ATR FT-IR spectroscopy, NMR spectroscopy, GPC and UV/VIS spectroscopy. The physical properties of polymers with different drug load were investigated using DSC, contact angle measurements and oscillatory rheology. Drug release was monitored over one month in vitro. A very slow, but continuous release was observed in PBS. Slightly acidic conditions and lipase activity are accelerating the indomethacin release. Therefore, poly(glycerol adipate) - indomethacin conjugates are promising prodrugs for the local sustained release of indomethacin.

Authors+Show Affiliations

Institute of Pharmacy, Martin Luther University Halle-Wittenberg, D-06099 Halle (Saale), Germany.Institute of Pharmacy, Pharmaceutical Technology, Leipzig University, D-04317 Leipzig, Germany.Institute of Chemistry, Martin Luther University Halle-Wittenberg, D-06099 Halle (Saale), Germany.Institute of Pharmacy, Martin Luther University Halle-Wittenberg, D-06099 Halle (Saale), Germany. Electronic address: karsten.maeder@pharmazie.uni-halle.de.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

28843347

Citation

Wersig, T, et al. "Poly(glycerol Adipate) - Indomethacin Drug Conjugates - Synthesis and in Vitro Characterization." International Journal of Pharmaceutics, vol. 531, no. 1, 2017, pp. 225-234.
Wersig T, Hacker MC, Kressler J, et al. Poly(glycerol adipate) - indomethacin drug conjugates - synthesis and in vitro characterization. Int J Pharm. 2017;531(1):225-234.
Wersig, T., Hacker, M. C., Kressler, J., & Mäder, K. (2017). Poly(glycerol adipate) - indomethacin drug conjugates - synthesis and in vitro characterization. International Journal of Pharmaceutics, 531(1), pp. 225-234. doi:10.1016/j.ijpharm.2017.08.093.
Wersig T, et al. Poly(glycerol Adipate) - Indomethacin Drug Conjugates - Synthesis and in Vitro Characterization. Int J Pharm. 2017 Oct 5;531(1):225-234. PubMed PMID: 28843347.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Poly(glycerol adipate) - indomethacin drug conjugates - synthesis and in vitro characterization. AU - Wersig,T, AU - Hacker,M C, AU - Kressler,J, AU - Mäder,K, Y1 - 2017/08/23/ PY - 2017/06/07/received PY - 2017/08/18/revised PY - 2017/08/20/accepted PY - 2017/8/28/pubmed PY - 2018/1/11/medline PY - 2017/8/28/entrez KW - Biodegradable polyesters KW - Biodegradable polymers KW - Drug conjugates KW - In vitro release KW - Indomethacin KW - Poly(glycerol adipate) KW - Rheology SP - 225 EP - 234 JF - International journal of pharmaceutics JO - Int J Pharm VL - 531 IS - 1 N2 - The linear biodegradable polyester poly(glycerol adipate) (PGA) was synthesized via enzymatic polycondensation using lipase B from Candida antarctica (CAL-B). Every monomer unit of PGA possesses a pendant hydroxyl group which is responsible for the hydrophilic character and moisture swelling. These OH groups were esterified to different degrees with the anti-inflammatory drug indomethacin in order to create a prodrug with a pH-sensitive linker for modified drug release. The structure of the conjugates was determined via ATR FT-IR spectroscopy, NMR spectroscopy, GPC and UV/VIS spectroscopy. The physical properties of polymers with different drug load were investigated using DSC, contact angle measurements and oscillatory rheology. Drug release was monitored over one month in vitro. A very slow, but continuous release was observed in PBS. Slightly acidic conditions and lipase activity are accelerating the indomethacin release. Therefore, poly(glycerol adipate) - indomethacin conjugates are promising prodrugs for the local sustained release of indomethacin. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/28843347/Poly_glycerol_adipate____indomethacin_drug_conjugates___synthesis_and_in_vitro_characterization_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(17)30811-6 DB - PRIME DP - Unbound Medicine ER -