A Novel Technique to Enhance Dissolution Rate of Cilnidipine Using Liquisolid Compact and Wet Granulation

Siju, V. V.; Soniwala, Moinuddin; Nagar, Swati

doi:10.25004/ijpsdr.2017.090402

Cited by 2 publications

(1 citation statement)

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“…It is a BCS Class II drug with aqueous solubility and oral bioavailability of 5.66×10 -3 mg/ml and 13 % respectively. 21 As per literature review, solid dispersion, 22 and liquisolid, 23 polymeric nanoparticles, 24 microemulsion, 25 and solid lipid nanoparticles, 26 have been used to enhance solubility and oral bioavailability of CLN. Bakhle et al 27 developed solid self emulsifying system of CLN using Capryol 90 as oil phase, Tween 80 as surfactant and Transcutol HP as cosurfactant but in vivo studies were not performed.…”

Section: Introductionmentioning

confidence: 99%

Self-nanoemulsifying Drug Delivery System of Cilnidipine

Rao¹,

Kulkarni²,

Sonawane³

et al. 2021

IJPER

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Aim: Self-nanoemulsifying Drug Delivery Systems (SNEDDS) are physically stable, isotropic mixtures of oil, surfactant and co-surfactant. The turbulence generated by peristaltic movements of the GIT causes formation of oil-in-water (o/w) nano-emulsions upon dilution. The objective of this study was to improve solubility and oral bioavailability of Cilnidipine by formulating liquid-SNEDDS. Materials and methods: Capmul PG8 NF, Cremophor RH40, and Transcutol HP were selected as oil, surfactant, and co-surfactant. Ternary phase diagrams were constructed to evaluate the nanoemulsification region. A 3 2 factorial design was employed to optimize L-SNEDDS with droplet size and drug release as responses. SNEDDS of CLN was evaluated for droplet size, self-emulsification time, in vitro drug release, ex-vivo permeation, pharmacokinetics and tissue distribution studies and stability studies. The optimized L-SNEDDS was converted into solid form using β-cyclodextrin nanosponges as adsorbents and evaluated in terms of micromeritics, drug content, scanning electron microscopy and powder X-ray diffraction. Results: The optimized batch exhibited droplet size of 23.70 nm, and in vitro drug release of 95.24 % in 60 min.The in-vivo studies revealed nearly 5.53 folds increase in AUC 0-∞ of optimized batch of liquid SNEDDS compared to CLN which can be credited to increase in solubility and dissolution rate. Conclusion: In vivo studies revealed improved pharmacokinetic properties which were attributed to greater surface area and lymphatic absorption leading to circumvention of hepatic first pass metabolism.

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