Influence of β-Cyclodextrin and Hydroxypropyl-β-Cyclodextrin on Enhancement of Solubility and Dissolution of Isradipine

DOI:

https://doi.org/10.37285/ijpsn.2017.10.3.8

Authors

  • Narendar D
  • Ettireddy S

Abstract

The content of this investigation was to study the influence of β-cyclodextrin and hydroxy propyl-β-cyclodextrin complexation on enhancement of solubility and dissolution rate of isradipine. Based on preliminary phase solubility studies, solid complexes prepared by freeze drying method in 1:1 molar ratio were selected and characterized by DSC for confirmation of complex formation. Prepared solid dispersions were evaluated for drug content, solubility and in vitro dissolution. The physical stability of optimized formulation was studied at refrigerated and room temperature for 2 months. Solid state characterization of optimized complex performed by DSC and XRD studies.  Dissolution rate of isradipine was increased compared with pure drug and more with HP-β-CD inclusion complex than β-CD. DSC and XRD analyzes that drug was in amorphous form, when the drug was incorporated as isradipine β-CD and HP-β-CD inclusion complex. Stability studies resulted in low or no variations in the percentage of complexation efficiency suggesting good stability of molecular complexes. The results conclusively demonstrated that the enhancement of solubility and dissolution rate of isradipine by drug-cyclodextrin complexation was achieved. 

 

Downloads

Download data is not yet available.

Metrics

Metrics Loading ...

Keywords:

Isradipine, complexation, β-cyclodextrin, hydroxypropyl-β-cyclodextrin, solubility, dissolution

Downloads

Published

2017-05-31

How to Cite

1.
D N, S E. Influence of β-Cyclodextrin and Hydroxypropyl-β-Cyclodextrin on Enhancement of Solubility and Dissolution of Isradipine. Scopus Indexed [Internet]. 2017 May 31 [cited 2024 Dec. 22];10(3):3752-7. Available from: https://ijpsnonline.com/index.php/ijpsn/article/view/848

Issue

Vol. 10 No. 3 (2017): May-June 2017

Section

Research Articles
Crossref
Scopus
Google Scholar
Europe PMC

References

Amidon GL, Lennernas H, Shah VP and Crison JR (1995). A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm Res 12(3): 413-420.
Chaumeil JC (1998). Micronization: a method of improving the bioavailability of poorly soluble drugs. Methods Find Exp Clin Pharmacol 20(3): 211-5.
Blagden N, de Matas M, Gavan PT and York P (2007). Crystal engineering of active pharmaceutical ingredients to improve solubility and dissolution rates. Adv Drug Deli Rev 59(7): 617-630.
Sinha S, Ali M, Baboota S, Ahuja A, Kumar A and Ali J (2010). Solid dispersion as an approach for bioavailability enhancement of poorly water-soluble drug ritonavir. AAPS Pharm Sci Tech 11(2): 518-527.
Rangel-Yagui CD, Pessoa A and Tavares LC (2005).Micellar solubilization of drugs. J Phar Pharmac Sci 8(2): 147-163.
Uekama K, Hirayama F, Irie T (1998). Cyclodextrin drug carrier systems.Chem Rev 98(5): 2045-2076.
Rogers TL, Hu J, Yu Z, Johnston KP and Williams RO (2002). A novel particle engineering technology: spray-freezing into liquid. Int J Pharm 242(1-2): 93-100.
Cao F, Guo J and Ping Q (2005).The physicochemical characteristics of freeze-dried scutellarin-cyclodextrin tetra component complexes. Drug Dev Ind Phar 31(8): 747-756.
Loftsson T and Brewster ME (1996). Pharmaceutical applications of cyclodextrins. Drug solubilization and stabilization. J Pharm Sci 85: 1017-1025.
Matsuda H and Arima H (1999). Cyclodextrins in transdermal and rectal delivery. Adv Drug Del Rev 36: 81-99.
Chrysant SG and Cohen M (1997). Long-term antihypertensive effects with chronic administration of isradipine controlled release. Curr Ther Res 58: 1-9.
Thirupathi G, Swetha E and Narendar D (2017). Role of isradipine loaded solid lipid nanoparticles in the pharmacodynamic effect of isradipine in rats. Drug res 67(03): 163-169.
De Waard H, Hinrichs W, Visser M, Bologna C and Frijlink H (2008). Differences in dissolution behavior of tablets prepared from solid dispersions with a surfactant physically mixed or incorporated. Int J Pharm 349(1-2): 66-73.
Gao X, Nishimura K, Hirayama F, Arima H, Uekama K, Schmid G, Terao K, Nakata D and Fukumi H (2006). Enhanced dissolution and oral bioavailability of coenzyme Q10 in dogs obtained by fusion complexation with c-cyclodextrin. Asian J Pharm Sci 1: 95-102.
Zeng J, Ren Y, Zhou C, Yu S and Chen WH (2011). Preparation andphysicochemical characteristics of the complex of edaravone with hydroxypropyl-β-cyclodextrin. Carbohyd Poly 83(3): 1101-5.
De Paula D, Oliveira DCR, Tedesco AC and Bentley MVLB (2007). Enhancing effectof modified beta-cyclodextrins on in vitro skin permeation of estradiol. Revista Brasileira de Ciências Farmacêuticas 43(1): 111-20.
Timko RJ and Lordi NG (1998). Thermal analysis studies of glass dispersion systems. Drug Dev Ind Pharm 10(3): 425-451.
Ramasahayam B, Eedara BB, Kandadi P, Jukanti R and Bandari S(2015). Development of isradipine loaded self-nano emulsifying powders for improved oral delivery: in vitro and in vivo evaluation. Drug Dev Ind Pharm 41(5): 753-63.