Characterization and in vivo evaluation of lacidipine inclusion complexes with β- cyclodextrin and its derivatives

Darekar, Titiksha and Shirodkar, Rupesh and Kumar, Lalit and Attari, Zenab and Lewis, Shaila (2016) Characterization and in vivo evaluation of lacidipine inclusion complexes with β- cyclodextrin and its derivatives. Journal of Inclusion Phenomena and Macrocyclic Chemistry, 84 (3). pp. 225-235. ISSN 1388-3127

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Abstract

The objective of the study was to explore the possible formation of the inclusion complex of lacidipine (LCDP), a class II drug under biopharmaceutics classification system (BCS) with beta-cyclodextrin (b-CD) andmodified b- CDs: hydroxy propyl- beta-cyclodextrin (HP-b-CD) and sulfobutyl ether-beta-cyclodextrin (SBE-b-CD) in order to enhance the solubility and the dissolution rate of the drugwith an intention to improve its bioavailability. The stability constants found using phase solubility studies showed that SBEb- CD formed themost stable inclusion complex with the drug (K = 348 ± 4 M-1) compared to the other cyclodextrins (CDs). The thermal analysis confirmed this finding. IR spectral analysis indicated the involvement of the hydroxyl function of CDs with the COOH of the drug. H1 NMR and 13C NMRspectral analysis indicated that the aromatic ring of drug included deeply in the CD cavity leaving the side chain protruding outside the CD cage and hydrogen bonds are formed which stabilizes the complex formation.The dissolution of the drug was improved on complexation with SBE-b-CD more effectively compared to the other CDs. The in vivo pharmacokinetic study of the complexes in Wistar rats showed an increase in AUC value by 1.5–2 times in case of (HP-b-CD) and SBE-b-CD compared to the plain drug and maximum with SBE-b-CD complex (Cmax = 242 ± 150 ng/ml, AUC = 1506.95 ± 0.505 ng/ml h).

Item Type: Article
Uncontrolled Keywords: Lacidipine; sulfobutyl ether b-cyclodextrin; solubility; complexation.
Subjects: Pharmacy > MCOPS Manipal > Pharmaceutics
Depositing User: KMC Library
Date Deposited: 21 May 2016 14:03
Last Modified: 21 May 2016 14:03
URI: http://eprints.manipal.edu/id/eprint/146102

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