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Effect of hydrophilic polymers on isradipine complexation with hydroxypropyl β-cyclodextrin.
Drug Dev Ind Pharm. 2013 Jul; 39(7):970-7.DD

Abstract

Complexation of isradipine with hydroxypropyl β-cyclodextrin (HPβCD) in the presence and absence of 3 hydrophilic polymers-polyvinyl pyrrolidone (PVP), hydroxypropyl methylcellulose (HPMC), and polyethylene glycol (PEG)-was investigated with an objective of evaluating the effect of hydrophilic polymers on the complexation and solubilizing efficiencies of HPβCD and on the dissolution rate of isradipine from the HPβCD complexes. The phase solubility studies indicated the formation of isradipine-HPβCD inclusion complexes at a 1:1M ratio in solution in both the presence and the absence of hydrophilic polymers. The complexes formed were quite stable. Addition of hydrophilic polymers markedly improved the complexation and solubilizing efficiencies of HPβCD. Solid inclusion complexes of isradipine-HPβCD were prepared in 1:1 and 1:2 ratios by the kneading method, with and without the addition of hydrophilic polymers. The solubility and dissolution rate of isradipine were significantly improved by complexation with HPβCD. The isradipine-HPβCD (1:2) inclusion complex yielded a 9.66-fold increase in the dissolution rate of isradipine. The addition of hydrophilic polymers also markedly improved the dissolution rate of isradipine from HPβCD complexes: a 11.72-, 17.01-, and 39.23-fold increase was observed with PVP, PEG, and HPMC respectively. X-ray diffractometry and differential scanning calorimetry indicated stronger drug amorphization and entrapment in HPβCD because of the combined action of HPβCD and the hydrophilic polymers.

Authors+Show Affiliations

Department of Pharmaceutical Technology, University College of Pharmaceutical Sciences, Andhra University, Visakhapatnam, India.No affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

22612875

Citation

Mummidi, Varalakshmi, and Vijayaratna Jayanthi. "Effect of Hydrophilic Polymers On Isradipine Complexation With Hydroxypropyl Β-cyclodextrin." Drug Development and Industrial Pharmacy, vol. 39, no. 7, 2013, pp. 970-7.
Mummidi V, Jayanthi V. Effect of hydrophilic polymers on isradipine complexation with hydroxypropyl β-cyclodextrin. Drug Dev Ind Pharm. 2013;39(7):970-7.
Mummidi, V., & Jayanthi, V. (2013). Effect of hydrophilic polymers on isradipine complexation with hydroxypropyl β-cyclodextrin. Drug Development and Industrial Pharmacy, 39(7), 970-7. https://doi.org/10.3109/03639045.2012.686508
Mummidi V, Jayanthi V. Effect of Hydrophilic Polymers On Isradipine Complexation With Hydroxypropyl Β-cyclodextrin. Drug Dev Ind Pharm. 2013;39(7):970-7. PubMed PMID: 22612875.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Effect of hydrophilic polymers on isradipine complexation with hydroxypropyl β-cyclodextrin. AU - Mummidi,Varalakshmi, AU - Jayanthi,Vijayaratna, Y1 - 2012/05/21/ PY - 2012/5/23/entrez PY - 2012/5/23/pubmed PY - 2013/11/10/medline SP - 970 EP - 7 JF - Drug development and industrial pharmacy JO - Drug Dev Ind Pharm VL - 39 IS - 7 N2 - Complexation of isradipine with hydroxypropyl β-cyclodextrin (HPβCD) in the presence and absence of 3 hydrophilic polymers-polyvinyl pyrrolidone (PVP), hydroxypropyl methylcellulose (HPMC), and polyethylene glycol (PEG)-was investigated with an objective of evaluating the effect of hydrophilic polymers on the complexation and solubilizing efficiencies of HPβCD and on the dissolution rate of isradipine from the HPβCD complexes. The phase solubility studies indicated the formation of isradipine-HPβCD inclusion complexes at a 1:1M ratio in solution in both the presence and the absence of hydrophilic polymers. The complexes formed were quite stable. Addition of hydrophilic polymers markedly improved the complexation and solubilizing efficiencies of HPβCD. Solid inclusion complexes of isradipine-HPβCD were prepared in 1:1 and 1:2 ratios by the kneading method, with and without the addition of hydrophilic polymers. The solubility and dissolution rate of isradipine were significantly improved by complexation with HPβCD. The isradipine-HPβCD (1:2) inclusion complex yielded a 9.66-fold increase in the dissolution rate of isradipine. The addition of hydrophilic polymers also markedly improved the dissolution rate of isradipine from HPβCD complexes: a 11.72-, 17.01-, and 39.23-fold increase was observed with PVP, PEG, and HPMC respectively. X-ray diffractometry and differential scanning calorimetry indicated stronger drug amorphization and entrapment in HPβCD because of the combined action of HPβCD and the hydrophilic polymers. SN - 1520-5762 UR - https://www.unboundmedicine.com/medline/citation/22612875/Effect_of_hydrophilic_polymers_on_isradipine_complexation_with_hydroxypropyl_β_cyclodextrin_ L2 - http://www.tandfonline.com/doi/full/10.3109/03639045.2012.686508 DB - PRIME DP - Unbound Medicine ER -