Preparationand In Vivo Evaluation Of A Self-Nanoemulsifying Drug Delivery System Loaded With Ceritinib
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Author:
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SUJITHA KATURI, BHIKSHAPATHI D.V.R.N
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Abstract:
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Objective: The present research deals with formulation of self-nanoemulsifying drug delivery system (SNEDDS) to improve the oral bioavailability of ceritinib.
Methods: Based on its maximum solubility an oil, surfactant and co-surfactant were chosen (captex355, tergitol and propylene glycol) and mixed in varying ratios for plotting pseudo tertiary phase diagram. Formulations that cleared stability tests were analyzed for % transmission, drug content and drug dissolution. The best formulation was characterized for FTIR, SEM, stability and pharmacokinetic studies.
Results: Formulation F13 with highest drug release of 98.9% in 60 min when compared to other formulations and pure drug (48 %) also displayed optimal particle size, Z average and zeta potential of 144 nm, 132 nm and -7.2 mV respectively. The FTIR and SEM analysis indicated no drug excipient interaction, confirming uniform drug distribution. The formulation was found stable for six months. The ceritinib SNEDDS displayed a significantly greater Cmax (65.54µg/mL) value than the pure drug suspension (21.05µg/mL) (P < 0.05) when administrated orally. The Tmax was 2.0h for SNEDDS while 4.0h for pure drug suspension. The comparative oral bioavailability of ceritinib in SNEDDS was 3.5-fold elevated when compared to pure suspension (P < 0.05).
Conclusion: The results indicate ceritinib SNEDDS formulations can be designed to augment the solubility of ceritinib and thereby increase in its absorption rate and drug release.
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Keyword:
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Ceritinib,oral bioavailability, self-nanoemulsifying drug delivery system, tergitol.
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EOI:
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-
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DOI:
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https://doi.org/10.31838/ijpr/2021.13.03.199
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