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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.


SEM photographs magnifications 200x at 10 kv (a) CA drug loaded nanocomposite microbeads (AF-3) and (b) CA-Neusilin US2 drug loaded nanocomposite microbeads (AF-7).
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fig6: SEM photographs magnifications 200x at 10 kv (a) CA drug loaded nanocomposite microbeads (AF-3) and (b) CA-Neusilin US2 drug loaded nanocomposite microbeads (AF-7).

Mentions: The SEM photomicrographs of the dried drug loaded CA nanocomposite microbeads are shown (Figure 6). Morphology of the drug loaded CA microbeads was discrete and spherical in shape with a rough outer surface and visible large wrinkles and pores having a sandy appearance due to less compactness (Figure 6(a)). In case of CA-Neusilin US2 nanocomposite microbeads are more spherical; absence of any pores, wrinkles, and also the drug is completely entrapped inside of the polymeric network due to interlocking of Neusilin US2 filler with SA gel (Figure 6(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)

SEM photographs magnifications 200x at 10 kv (a) CA drug loaded nanocomposite microbeads (AF-3) and (b) CA-Neusilin US2 drug loaded nanocomposite microbeads (AF-7).
© Copyright Policy - open-access
Related In: Results  -  Collection

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

fig6: SEM photographs magnifications 200x at 10 kv (a) CA drug loaded nanocomposite microbeads (AF-3) and (b) CA-Neusilin US2 drug loaded nanocomposite microbeads (AF-7).
Mentions: The SEM photomicrographs of the dried drug loaded CA nanocomposite microbeads are shown (Figure 6). Morphology of the drug loaded CA microbeads was discrete and spherical in shape with a rough outer surface and visible large wrinkles and pores having a sandy appearance due to less compactness (Figure 6(a)). In case of CA-Neusilin US2 nanocomposite microbeads are more spherical; absence of any pores, wrinkles, and also the drug is completely entrapped inside of the polymeric network due to interlocking of Neusilin US2 filler with SA gel (Figure 6(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.