Formulation and Evaluation of Meloxicam Hybrid nano Particles

The goal of the present study was to prepare meloxicam (MX) entrapped hybrid particles (HPs) to enhance intestinal permeation and anti-inflammatory activity. MX-HPs were prepared by nanoprecipitation method using lipid, chitosan, poloxamer, and TPGS. The formulations (MX-HPs1, MX-HPs2, MX-HPs3) were evaluated for particle size, entrapment efficiency, and drug release to select the optimized composition and further evaluated for permeation study, stability study, morphology, interaction study, and anti-inflammatory activity by carrageenan-induced rat paw edema test. The prepared MX-HPs showed nano sized particles (198.5 ± 3.7 to 223.8 ± 2.1 nm) and PDI (<0.3), zeta potential (16.5 ± 2.7 to 29.1 ± 3.6 mV), and high entrapment efficiency (75.1 ± 4.7 to 88.5 ± 3.9%). The surface morphology was assessed by transmission electron microscopy and showed non-aggregated particles. Infra-red (IR) spectroscopy of pure MX as well as formulation revealed no drug-polymer interaction and X-ray diffraction confirmed the conversion of crystalline MX into amorphous form. The release study data revealed prolonged MX release for 24 h. The selected optimized hybrid particles (MX-HPs2) revealed a 2.3-fold improved enhancement ratio than free MX. The storage stability and gastrointestinal stability data demonstrated a stable formulation in SIF as well as SGF. The anti-inflammatory activity showed better therapeutic action than pure MX dispersion. From the study, it can be concluded that the prepared MX-HPs may be a promising delivery system for MX in treating inflammatory disorders.

Materials

The gift sample of Meloxicam (MX) was provided by M/s Lupin Pharmaceuticals Ltd., Goa, India. Chitosan and Vitamin E TPGS were purchased from Sigma Aldrich, Saint Louis, Missouri, USA. Stearic acid, Ethanol, Chloroform and Poloxamer 188 procured from Thermo Fisher Scientific, Mumbai, India and Alpha Aesar, UK. The other ingredients and solvents used were of analytical grade. Wistar albino rats (200–250 gm; either sex) were used in the animal experi-ment. The ethical approval was taken from Bilwal Medchem and Research Laboratory Pvt. Ltd. in Jaipur, Rajasthan, India (Registration No. 2005/PO/RcBT/S/18CPCSEA). The approved study protocol number (BMRL/IAEC/2021-54) from animal ethics committee.

Read more

Asif, M., Fatima, K., Imam, S.S. et al. Formulation and Evaluation of Meloxicam Hybrid nano Particles. AAPS PharmSciTech 25, 172 (2024).
https://doi.org/10.1208/s12249-024-02878-8

See also the video on TPGS