pH Responsive Hydrogels for the Delivery of Capecitabine: Development, Optimization and Pharmacokinetic Studies

The objective of the current study was to achieve a sustained release profile of capecitabine (CAP), an anticancer agent frequently administered in conventional dosage form due to its short plasma half-life. A drug-loaded smart pH responsive chitosan/fenugreek-g-poly (MAA) hydrogel was synthesized b...

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Bibliographic Details
Published in:Gels 2022-11, Vol.8 (12), p.775
Main Authors: Rehman, Umaira, Sarfraz, Rai Muhammad, Mahmood, Asif, Akbar, Shehla, E Altyar, Ahmed, Khinkar, Roaa M, Gad, Heba A
Format: Article
Language:English
Subjects:
Anticancer properties
Biocompatibility
Cancer
Capecitabine
Chitosan
Colorectal cancer
Controlled release
drug discovery
Free radical polymerization
Free radicals
Half-life
health care
hydrogel
Hydrogels
Optimization
Patient compliance
pharmacokinetic
Pharmacokinetics
Pharmacology
Physiology
Polymerization
Polymers
Scanning electron microscopy
Spectrum analysis
Sustained release
Swelling
Toxicity
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Summary:The objective of the current study was to achieve a sustained release profile of capecitabine (CAP), an anticancer agent frequently administered in conventional dosage form due to its short plasma half-life. A drug-loaded smart pH responsive chitosan/fenugreek-g-poly (MAA) hydrogel was synthesized by an aqueous free radical polymerization technique. The developed network was evaluated for capecitabine loading %, swelling response, morphology, structural and compositional characteristics, and drug release behavior. Significantly higher swelling and in vitro drug release rate were exhibited by formulations at pH 7.4 than at pH 1.2, demonstrating the pH responsive character of hydrogels. Swelling percentage and CAP loading ranged within 74.45-83.54% and 50.13-72.43%, respectively. Maximum release, up to 93%, was demonstrated over 30 h, evidencing the controlled release pattern of CAP from hydrogels. The optimized formulation was further screened for acute oral toxicity studies. No signs of oral, dermal, or ocular toxicities were noticed, confirming safety evidence of the network. Furthermore, pharmacokinetic analysis demonstrated the sustained release response of CAP from hydrogels as confirmed by a significant increase in plasma half-life (t ) (13 h) and AUC (42.88 µg h/mL) of CAP. Based on these findings, fabricated hydrogels are strongly recommended as a biocompatible carrier for colorectal delivery of active agents.
ISSN:2310-2861
2310-2861
DOI:10.3390/gels8120775