Journal
ARTIFICIAL CELLS NANOMEDICINE AND BIOTECHNOLOGY
Volume 47, Issue 1, Pages 144-153Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1080/21691401.2018.1546186
Keywords
Asenapine maleate; solid lipid nanoparticles; Caco-2 cell line; bioavailability; oral absorption mechanism; lymphatic transport
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Funding
- Department of Science and Technology (DST), New Delhi, India
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The aim of the present investigation was to fabricate and evaluate solid lipid nanoparticles (SLNs) of asenapine maleate (AM) to improve its oral bioavailability (BA). AM-SLNs were prepared by high speed homogenization followed by ultrasonication technique. The resultant SLNs exhibited particle size, zeta potential and entrapment efficiency of 114.3 +/- 3.5nm, -12.9 +/- 3.8mV, and 84.10%+/- 2.90% respectively. In vitro release study of AM-SLNs showed 9.23%+/- 2.72% and 92.09%+/- 3.40% release of AM in pH 1.2 medium and phosphate buffer pH 6.8, respectively, indicating higher potential of lymphatic uptake. Cell viability study using Caco-2 cell line indicated non-toxicity of the carriers and drug. The uptake of AM-SLNs across Caco-2 cell line was time and energy dependent exhibiting clathrin-claveole mediated endocytosis transport. Cellular uptake of Coumarin loaded SLNs was effectively increased as compared to the dye solution. The pharmacokinetic results in rats showed 50.19-fold improvement in BA of AM after fabrication of SLNs. Collectively, all these findings demonstrated effectiveness of SLNs to improve therapeutic efficacy of AM in the treatment of schizophrenia.
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