Related Experiment Video
Updated: Aug 26, 2025
Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
Published on: August 28, 2015
Meloxicam loaded hydroxypropyl methylcellulose (HPMC) microparticulate: Fabrication, characterization and in vivo
Syed Abdul Wasay1, Syed Umer Jan1, Muhammad Akhtar2
1Faculty of Pharmacy and Health Sciences, University of Balochistan, Quetta, Pakistan.
Abstract:
Meloxicam (MEL) is an oxicam derivative with low water solubility that is useful in the treatment of colorectal cancer (CRC) as a COX-2 inhibitor. MEL-loaded HPMC micro particles were fabricated using an oil-in-oil (o/o) emulsion solvent evaporation (ESE) method. FTIR, XRD, particle size analysis, DSC, SEM and in vitro dissolution investigation were utilized to evaluate the produced micro particles physiochemically. Finally, rabbits were used as animal models in an in vivo pharmacokinetic study to assess the MEL concentration in the plasma of rabbits. Pure MEL, F1 and F2 were given to rabbits by a single dose for in vivo pharmacokinetic investigations. The XRD and DSC results confirmed the transformation of MEL from its crystalline nature to the amorphous state in micro particles. The formulations F1 and F2 particle sizes were determined 92.43μm and 163.26μm, respectively. The prepared micro particles had a smooth, non-porous and spherical surface. In comparison to the pure drug (22.4%), the F1 and F2 cumulative drug release (%) was 86.19% and 79.57%, respectively. Pure MEL, F1 and F2 have estimated Cmax values of 7.21, 25.41 and 22.38μg/mL, respectively. MEL had a half-life of 19.98 hours, which rose to 22.19 hours and 24.75 hours for F1 and F2, respectively. MEL, F1 and F2 had AUC0-α values of 116.034, 445.95 and 462.72μg/mL*h, respectively. Considering these aspects, MEL-loaded HPMC micro particles may have the potential to better the delivery and control the release of drug that is not easily dissolved in water which could lead to improved therapeutic efficacy and limited side effects.
Insights
This study developed meloxicam (MEL)-loaded HPMC microparticles using an emulsion solvent evaporation method. These microparticles improved MEL
Area of Science:
- Pharmaceutical Sciences
- Materials Science
- Drug Delivery
Background:
- Meloxicam (MEL) is an oxicam derivative used for colorectal cancer (CRC) treatment, acting as a COX-2 inhibitor.
- MEL exhibits low water solubility, posing challenges for effective drug delivery and therapeutic outcomes.
- Developing advanced formulations is crucial to enhance MEL's bioavailability and efficacy.
Purpose of the Study:
- To fabricate and characterize meloxicam-loaded hydroxypropyl methylcellulose (HPMC) microparticles.
- To evaluate the physicochemical properties and in vitro drug release of the MEL-loaded microparticles.
- To assess the in vivo pharmacokinetic profile of MEL-loaded microparticles in a rabbit model.
Main Methods:
- Meloxicam-loaded HPMC microparticles were prepared using an oil-in-oil (o/o) emulsion solvent evaporation (ESE) technique.
- Physicochemical characterization involved FTIR, XRD, particle size analysis, DSC, and SEM.
- In vitro dissolution studies and in vivo pharmacokinetic assessments in rabbits were conducted.
Main Results:
- XRD and DSC confirmed the conversion of crystalline MEL to an amorphous state within the microparticles.
- Particle sizes for F1 and F2 formulations were 92.43μm and 163.26μm, respectively, with smooth, spherical surfaces.
- In vitro drug release for F1 and F2 was significantly higher (86.19% and 79.57%) compared to pure MEL (22.4%).
- In vivo studies showed increased Cmax, half-life, and AUC0-α for MEL-loaded microparticles compared to pure MEL, indicating enhanced bioavailability.
Conclusions:
- MEL-loaded HPMC microparticles demonstrate potential for improved delivery of poorly water-soluble drugs.
- The developed microparticles offer controlled release, potentially leading to enhanced therapeutic efficacy.
- This formulation strategy may reduce side effects associated with conventional MEL administration.
More Related Videos
10:53Anionic Polymerization of an Amphiphilic Copolymer for Preparation of Block Copolymer Micelles Stabilized by π-π Stacking Interactions
Published on: October 10, 2016
09:57A Facile and Efficient Approach for the Production of Reversible Disulfide Cross-linked Micelles
Published on: December 23, 2016
Related Concept Videos
01:28Factors Influencing Drug Absorption: Pharmaceutical Parameters
01:21Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism
Some polymorphic crystals possess lower aqueous solubility than their amorphous counterparts, leading to incomplete absorption. For instance, the oral suspension of Chloramphenicol, which...
01:20Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry