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

Mallappa MK, Kesarla R, Banakar S - J Drug Deliv (2015)

Bottom Line: 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.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.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, TVM College of Pharmacy, Bellary, Karnataka, India.

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.

No MeSH data available.


(a) Effect of SA on mechanical strength of CA nanocomposite microbeads. (b) Effect of Neusilin on mechanical strength of CA nanocomposite microbeads.
© Copyright Policy - open-access
Related In: Results  -  Collection


getmorefigures.php?uid=PMC4352939&req=5

fig7: (a) Effect of SA on mechanical strength of CA nanocomposite microbeads. (b) Effect of Neusilin on mechanical strength of CA nanocomposite microbeads.

Mentions: The maximum force for 50% displacement or breakdown was used to evaluate the strength of the microbeads. The mechanical strength of the CA nanocomposite microbeads was increased by increasing the concentration of SA in the formulation (Figure 7(a)). The maximum force for 50% displacement of the microbeads gradually increased with increasing concentration of Neusilin US2 content. The content of Neusilin US2 above 1.5% w/w did not show any greater changes in the strength of the beads due to complete saturation level of Neusilin US2 with SA. This result indicated that the Neusilin US2 interacts with SA adsorbing oil and water content in interior level of the beads during the cross-linking process and could create a dense matrix structure that reinforced the strength of the microbeads (Figure 7(b)).


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

Mallappa MK, Kesarla R, Banakar S - J Drug Deliv (2015)

(a) Effect of SA on mechanical strength of CA nanocomposite microbeads. (b) Effect of Neusilin on mechanical strength of CA nanocomposite microbeads.
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4352939&req=5

fig7: (a) Effect of SA on mechanical strength of CA nanocomposite microbeads. (b) Effect of Neusilin on mechanical strength of CA nanocomposite microbeads.
Mentions: The maximum force for 50% displacement or breakdown was used to evaluate the strength of the microbeads. The mechanical strength of the CA nanocomposite microbeads was increased by increasing the concentration of SA in the formulation (Figure 7(a)). The maximum force for 50% displacement of the microbeads gradually increased with increasing concentration of Neusilin US2 content. The content of Neusilin US2 above 1.5% w/w did not show any greater changes in the strength of the beads due to complete saturation level of Neusilin US2 with SA. This result indicated that the Neusilin US2 interacts with SA adsorbing oil and water content in interior level of the beads during the cross-linking process and could create a dense matrix structure that reinforced the strength of the microbeads (Figure 7(b)).

Bottom Line: 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.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.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, TVM College of Pharmacy, Bellary, Karnataka, India.

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.

No MeSH data available.