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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 cummulative percentage of drug release from CA nanocomposite microbeads. (b) Effect of Neusilin US2 on cummulative percentage of drug release from CA nanocomposite microbeads. (c) Effect of calcium chloride on cummulative percentage of drug release from CA-Neusilin US2 nanocomposite microbeads.
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fig8: (a) Effect of SA on cummulative percentage of drug release from CA nanocomposite microbeads. (b) Effect of Neusilin US2 on cummulative percentage of drug release from CA nanocomposite microbeads. (c) Effect of calcium chloride on cummulative percentage of drug release from CA-Neusilin US2 nanocomposite microbeads.

Mentions: ACF-Na has been slightly soluble in water and showed very poor solubility in the acidic buffer media. However, the percentage of drug release from CA nanocomposite microbeads [AF-1 to AF-4] in SGF pH 1.2 within 2 h in the range of 32.54, 30.56, 28.35, and 26.55 w/w may be due to the stability of alginate at lower pHs and conversion of calcium alginate to the insoluble alginic acid to form tightening of the gel mesh work. On the other hand, the percentage of drug release in pH 6.8 PBS at 6 h is shown in the range of 52.33, 49.52, 44.25, and 37.65 w/w. Further, the percentage of drug release from microbeads in pH 7.4 SIF up to 12 h is 99.65, 97.12, 95.45, and 89.12 w/w (Figure 8(a)). As the concentration of SA increased, release rate of ACF-Na from the nanocomposite microbeads decreased, which shows biphasic pattern; that is, an initial rapid release (burst effect) phase was followed by a second slower drug release phase. The first phase might be disintegration of alginate in the presence surfactant and cosurfactant mainly based on drug diffusion through the small pores and cracks. The second phase exhibited slow release pattern, which was accompanied by diffusivity of polymer relaxation due to change in pH of the medium. The SA concentration in the formulation greatly influenced the steady state release of drug from the nanocomposite microbeads.


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 cummulative percentage of drug release from CA nanocomposite microbeads. (b) Effect of Neusilin US2 on cummulative percentage of drug release from CA nanocomposite microbeads. (c) Effect of calcium chloride on cummulative percentage of drug release from CA-Neusilin US2 nanocomposite microbeads.
© Copyright Policy - open-access
Related In: Results  -  Collection

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

fig8: (a) Effect of SA on cummulative percentage of drug release from CA nanocomposite microbeads. (b) Effect of Neusilin US2 on cummulative percentage of drug release from CA nanocomposite microbeads. (c) Effect of calcium chloride on cummulative percentage of drug release from CA-Neusilin US2 nanocomposite microbeads.
Mentions: ACF-Na has been slightly soluble in water and showed very poor solubility in the acidic buffer media. However, the percentage of drug release from CA nanocomposite microbeads [AF-1 to AF-4] in SGF pH 1.2 within 2 h in the range of 32.54, 30.56, 28.35, and 26.55 w/w may be due to the stability of alginate at lower pHs and conversion of calcium alginate to the insoluble alginic acid to form tightening of the gel mesh work. On the other hand, the percentage of drug release in pH 6.8 PBS at 6 h is shown in the range of 52.33, 49.52, 44.25, and 37.65 w/w. Further, the percentage of drug release from microbeads in pH 7.4 SIF up to 12 h is 99.65, 97.12, 95.45, and 89.12 w/w (Figure 8(a)). As the concentration of SA increased, release rate of ACF-Na from the nanocomposite microbeads decreased, which shows biphasic pattern; that is, an initial rapid release (burst effect) phase was followed by a second slower drug release phase. The first phase might be disintegration of alginate in the presence surfactant and cosurfactant mainly based on drug diffusion through the small pores and cracks. The second phase exhibited slow release pattern, which was accompanied by diffusivity of polymer relaxation due to change in pH of the medium. The SA concentration in the formulation greatly influenced the steady state release of drug from the nanocomposite microbeads.

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.