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Bosentan loaded Nano structured lipid carriers: A novel formulation and evaluation of their In-vitro, Ex-vivo and In-vivo characteristic using 3 full factorial design.
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| Author:
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DR. PRAJAPATI, MR. UMANG VARIA
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| Abstract:
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This study carried out to improve bioavailability and reduce dose frequency of Bosentan, because of drug accumulation
due to conventional therapy it cause serious liver toxicity. Bosentan loaded nanostructured lipid carriers
(NLCs)
prepared by using high-speed homogenization followed by an ultra-sonication. Optimization done by response surface
methodology to identify the effect of solid to liquid lipid ratio
(X1
) and surfactant strength
(X2
) on the particle size
(Y1
)
and drug loading
(Y2
). From the Preformulation study Precirol ATO 5, Transcutol HP and Poloxamer 188 selected as a
solid lipid, liquid lipid and surfactant, respectively. Optimize formula having solid to liquid lipid ratio
(85:15
) %w/w and
surfactant strength 1% w/v. Final formulation contained particle size 144.5±0.34 nm
(n=3
), surface charge -36.6 mv and
90.89±0.10 % (n=3
) drug entrapment. Characterization performed using DSC, FTIR and TEM analysis. The Haemolytic
study carried out to check blood compatibility. In- Vitro and Ex -Vivo drug release study shows 93.36% and 88.87 %,
respectively after 24 hours. In-vivo Performance was conducted on wistar Albino rats. As per the result of in-vivo study
pharmacokinetic parameters were quite different for Conventional formulation and NLCs. Bosentan NLCs absorb
through the lymphatic system containing Peyer’s patches. Optimize stable formulation gives the controlled release
according to Fick’s law. As uptake of Bosentan NLCs through Peyer’s patches it may improve the bioavailability of the
drug and reduce the liver toxicity.
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| Keyword:
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NLC; Surface response methodology; Haemolytic study; Hot homogenization technique, In-vivo study.
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| EOI:
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-
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| DOI:
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https://doi.org/10.31838/ijpr/2020.12.01.005
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| Download:
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