Effect of hydrogen bond formation/replacement on solubility characteristics, gastric permeation and pharmacokinetics of curcumin by application of powder solution technology.
- Author:
Vijay SHARMA
1
;
Kamla PATHAK
1
Author Information
1. Department of Pharmaceutics, Rajiv Academy for Pharmacy, Delhi - Mathura Road, Mathura 281001, Uttar Pradesh, India.
- Publication Type:Journal Article
- Keywords:
Bioavailability;
Curcumin;
Cytotoxicity;
Gastric permeation;
Hydrogen bond formation;
Liquisolid tablet;
Pharmacokinetics;
Powder solution technology
- From:
Acta Pharmaceutica Sinica B
2016;6(6):600-613
- CountryChina
- Language:English
-
Abstract:
The present research aimed to improve the dissolution rate and bioavailability of curcumin using the potential of liquisolid technology. Twelve drug-loaded liquisolid systems (LS-1 to LS-12) were prepared using different vehicles (PEG 200, PEG 400 and Tween 80) and curcumin concentrations in vehicle (40%, 50%, 60% and 70%,/). The carrier [microcrystalline cellulose (MCC) PH102] to coat (Aerosil) ratio was 20 in all formulations. The systems were screened for pre-compression properties before being compressed to liquisolid tablets (LT-1 to LT-12). Post compression tests anddissolution of LTs were conducted and the results compared with those obtained for a directly compressed tablet (DCT) made of curcumin, MCC PH102 and Aerosil. LTs exhibited higher cumulative drug release (CDR) than the DCT and the optimum formulation, LT-9 (made using Tween 80), was studied by powder XRD, DSC, SEM and FTIR.permeation of curcumin from LT-9 through goat gastrointestinal mucosa was significantly (<0.05) enhanced and its oral bioavailability was increased 18.6-fold in New Zealand rabbits.cytotoxicity (IC) of LT-9 towards NCL 87 cancer cells was 40.2 µmol/L substantiating its anticancer efficacy. Accelerated stability studies revealed insignificant effects of temperature and humidity on LT-9. In summary, solubility enhancement of curcumin in LTs produced significant improvements in its permeation and bioavailability.
