Calcium Alginate-Neusilin US2 Nanocomposite Microbeads for Oral Sustained Drug Delivery of Poor Water Soluble Drug Aceclofenac Sodium

Abstract

The aim of the present study was to formulate and investigate the calcium alginate- (CA-) Neusilin US2 nanocomposite microbeads containing preconcentrate of aceclofenac sodium (ACF-Na) liquid microemulsion (L-ME) for enhancement of oral bioavailability. The preconcentrate L-ME is prepared by using Labrafac PG, Labrasol, and Span 80 as oil, surfactant, and cosurfactant, respectively. The solid CA nanocomposite microbeads of L-ME prepared by microemulsification internal gelation technique using sodium alginate (SA) gelling agent, Neusilin US2 as adsorbent, and calcium chloride as crosslinking agent. L-ME has good thermodynamic stability; globule size was found to be 32.4 nm with polydispersity index 0.219 and −6.32 mV zeta potential. No significant interactions of excipients, drug in the formulations observed by FT-IR, DSC and XPRD. The concentration of SA and Neusilin US2 influences the flow properties, mean particle size, mechanical strength, drug entrapment efficiency, and percentage of drug release. All the formulations show minimum drug release in simulated gastric fluid (SGF) pH 1.2 for initial 2 h, maximum drug release in pH 6.8 phosphate buffer solution (PBS) at 6 h, followed by sustaining in simulated intestinal fluid (SIF) of pH 7.4 up to 12 h. The interaction of SA with Neusilin US2 creates a thick thixotropic gel network structure which acts as barrier to control the release of drug in the alkaline pH environment. Neusilin US2 is a novel filler used to convert L-ME into solid nanocomposite microbeads to enhance dissolution rate of poor water soluble drugs sustaining the drug release for prolonged period of time.

Microfluidic‐Spinning‐Directed Microreactors Toward Generation of Multiple Nanocrystals Loaded Anisotropic Fluorescent Microfibers

“…The solidified Ca‐alginate fibers were then extruded through an outlet channel and collected continuously (see Video S1, Supporting Information). These decreases in the intensities of CO (1025 cm −1 ) and the CH (2926 cm −1 ) stretching peak of Ca‐alginate, as shown in the FT‐IR and IR images (Figure c), further confirm the ionic crosslinking between the Ca 2+ and SA . We also fabricated NCs loaded fluorescent hybrid microfibers by incorporating different‐sized CdTe NCs into the SA core flow (Figure b).…”

Controlled release of nisin from Neusilin particles to enhance food safety of sour curd cheese

“…Thus, the highly porous Neusilin was employed as carrier material for controlled slow release of adsorbed nisin to minimize its food interaction and exposition to degradation. Different Neusilin types were previously applied as excipient and improved solubility of less water soluble drugs (Mallappa et al 2015). Hence, the poor solubility of nisin at neutral pH was circumvented by UFL2.…”

“…Particles such as Neusilin are chemical and physical robust candidates as adsorption material in innovative food protection systems and are based on magnesium aluminometasilicate. Neusilin particles were successfully used as excipient in pharmaceutical formulations (Mallappa et al 2015), as an adsorbent powder in animal feed administration (Ma et al 2016), nutritional supplementation (Santaniello and Giannini 2016) and were already approved by US Food and Drug Administration as drug master file. Moreover, Neusilin provide several advantages such as adjustable size, large surface area, pH-dependent release, and reduced interactions to food components of adsorbed nisin as well as reduced microbial enzymatic degradation (Aasen et al 2003;Bhatti et al 2004;Chollet et al 2008;Sun et al 2009).…”

Formulation and Evaluation of Carbamazepine Liquisolid Compacts Using Novel Carriers

“…35 Liquisolid compact containing Neusilin showed good compactibility, due to its high specific surface area and porosity. 36…”