Encapsulation of Naproxen in Lipid-Based Matrix Microspheres: Characterization and Release Kinetics

Abstract

The objective of this study was to microencapsulate the anti-inflammatory drug (naproxen) to provide controlled release and minimizing or eliminating local side effect by avoiding the drug release in the upper gastrointestinal track. Naproxen was microencapsulated with lipid-like carnauba wax, hydrogenated castor oil using modified melt dispersion (modified congealable disperse phase encapsulation) technique. Effect of various formulation and process variables such as drug-lipid ratio, concentration of modifier, concentration of dispersant, stirring speed, stirring time, temperature of external phase, on evaluatory parameters such as size, entrapment efficiency, and in vitro release of naproxen were studied. The microspheres were characterized for particle size, scanning electron microscopy (SEM), FT-IR spectroscopy, drug entrapment efficiency, in vitro release studies, for in vitro release kinetics. The shape of microspheres was found to be spherical by SEM. The drug entrapment efficiency of various batches of microspheres was found to be ranging from 60 to 90 %w/w. In vitro drug release studies were carried out up to 24 h in pH 7.4 phosphate buffer showing 50-65% drug release. In vitro drug release from all the batches showed better fitting with the Korsmeyer-Peppas model, indicating the possible mechanism of drug release to be by diffusion and erosion of the lipid matrix.

Development of Smart Polymer Microparticles through Suspension Polymerization for Treatment of Schistosomiasis

“…Among the many available controlled release systems, the successful use of polymer microparticles has been reported in the literature in distinct biomedical applications . Microparticles are characterized by characteristic sizes ranging from 1 to 1000 µm and can be applied in the form of microspheres or microcapsules: while microspheres are constituted by compact polymer matrixes (which may contain a dispersed drug), microcapsules are constituted by a rigid polymer wall that surrounds a core of distinct composition (where the drug is usually present)…”

Sustained-release of naproxen sodium from electrospun-aligned PLLA-PCL scaffolds

“…Despite the successful fabrication of scaffolds with the desired morphological properties for tendon TE, the major issue still lies in the ability to control the release of NPS in preventing adhesion formation. To address this, several attempts, such as the loading of NPS into PLGA microspheres, lipid‐like carnauba wax microparticles, Eudragit S‐100‐coated sodium alginate microspheres and electrospun cellulose acetate scaffolds, had been reported (Bhoyar et al, ; Bozdag et al, ; Simonoska Crcarevska et al, ). However, so far, these systems have only been able to achieve short NPS release profiles, from a few hours to a few days, due to the very hydrophilic nature and low molecular weight of NPS.…”

“…However, drawbacks, such as inadequate mechanical properties and a rapid release of NPS, have limited their application in tissue engineering (Aher et al, ; Bae and Kim, ; Bhise et al, ; Cifkova et al, ). On the other hand, other attempts in releasing NPS from hydrophobic matrices (Bhoyar et al, ; Bozdag et al, ; Simonoska Crcarevska et al, ) were also not entirely successful, mainly due to the hydrophilicity and low molecular weight of NPS.…”

Development of Novel Microstructured Lipid Carriers for Dissolution Rate Enhancement of Albendazole

“…The use of lipid materials as a matrix for microspheres can have some advantages. For example, these kinds of materials are usually biocompatible, biodegradable, non-immunogenic, and they are not expensive [2]. One of their main advantages is that they allow to encapsulate a great variety of non-water soluble compounds [2][3][4].…”

“…For example, these kinds of materials are usually biocompatible, biodegradable, non-immunogenic, and they are not expensive [2]. One of their main advantages is that they allow to encapsulate a great variety of non-water soluble compounds [2][3][4]. Among these compounds, these carriers could be useful to the class II drugs according to the Biopharmaceutical Classification System, which are characterized by showing a low aqueous solubility and high membrane permeability.…”