1Lecturer, Department of Pharmacy, Government Polytechnic, Visakhapatnam, Andhra Pradesh, India
2Associate Professor, Department of Pharmaceutical Technology, Aditya College of Pharmacy, Surampalem, Kakinada, India
3Assistant Professor, Department of Allied Health Science, Saraswati College of Pharmacy, SGC Group, Gharuan, Mohali, Punjab, India
4Assistant Professor, University School of Pharmaceutical Sciences, Rayat Bahra University, Mohali, Punjab, India
5Assistant Professor, Department of Pharmaceutical Chemistry, Parul Institute of Pharmacy, Parul University, Vadodara, Gujarat, India
6Professor, Department of Pharmacology, Chandigarh College of Pharmacy, Mohali, Punjab, India
7Assistant Professor, Department of Pharmaceutics, Guru Nanak Institute of Pharmacy, Dalewal, Hoshiarpur, Punjab, India
8Department of Pharmacy, Institute of Biomedical Education and Research, Mangalayatan University, Aligarh, India
9*Professor, Department of Pharmaceutics, Sardar Patel College of Pharmacy, Bakrol, Anand, Gujarat, India
Background: Piroxicam is a potent non-steroidal anti-inflammatory drug (NSAID) widely used for the management of inflammatory disorders. However, its long-term administration is associated with significant gastric irritation and ulceration due to direct mucosal contact and prostaglandin inhibition. Prodrug modification and nanocarrier-based delivery systems represent promising strategies to enhance therapeutic safety and sustain pharmacological activity.
Objective: The present study aimed to design and synthesize a piroxicam ester prodrug and incorporate it into a chitosan–gold nanocomposite carrier system to achieve sustained anti-inflammatory activity with reduced gastric toxicity.
Materials and Methods: The piroxicam ester prodrug was synthesized via esterification and characterized using FTIR, ¹H-NMR, and lipophilicity (LogP) analysis. The prodrug was incorporated into a Chitosan–Gold nanoparticles nanocomposite system prepared by ionic gelation and in situ reduction method. The formulation was evaluated for particle size, zeta potential, morphology (SEM and TEM), drug loading efficiency, and in vitro release profile. In vivo anti-inflammatory activity was assessed using carrageenan-induced paw edema model in rats, and gastric toxicity was evaluated through ulcer index determination and histopathological examination.
Results: Spectral data confirmed successful ester formation with increased lipophilicity compared to pure piroxicam. The optimized nanocomposite exhibited nanoscale particle size (~120–150 nm), positive surface charge, and high encapsulation efficiency (>80%). In vitro release studies demonstrated sustained drug release over 24 hours following Higuchi diffusion kinetics. In vivo studies revealed significantly enhanced and prolonged inhibition of paw edema for the nanocomposite formulation compared to pure drug (p < 0.05). Gastric toxicity studies showed a marked reduction in ulcer index and improved mucosal integrity in histopathological sections, indicating substantial gastroprotective effect.
Conclusion: The developed piroxicam ester prodrug-loaded chitosan–gold nanocomposite successfully achieved sustained anti-inflammatory activity with significantly reduced gastric toxicity. This integrated prodrug–nanocarrier strategy demonstrates improved pharmacological performance and holds strong potential for future pharmacokinetic evaluation and clinical translation.
Keywords: Piroxicam ester prodrug; Chitosan–gold nanocomposite; Sustained release; Anti-inflammatory activity; Gastric toxicity; Nanocarrier drug delivery
How to cite this article: Batna JR, Janipalli AP, Kumar P, Sharma SK, Patel N, Neekhra S, Kaur H, Khurshid F, Bhura MR. Design and Evaluation of Piroxicam Ester Prodrug Incorporated in Chitosan–Gold Nanocomposite Carriers for Sustained Anti-Inflammatory Activity and Reduced Gastric Toxicity. Int J Drug Deliv Technol. 2026;16(11s): 20-30; DOI: 10.25258/ijddt.16.11s.3
Source of support: Nil.
Conflict of interest: None