Development and optimization of Ropinirole loaded self-nanoemulsifying tablets

Background

The present research work aims to develop a Ropinirole-loaded self-Nanoemulsifying Drug Delivery system. Ropinirole has limited oral bioavailability due to substantial first-pass metabolism, which ultimately results in poor oral bioavailability and reduces plasma drug concentration and an overall reduction in therapeutic effects. Avoiding hepatic first-pass metabolism by increasing lymphatic uptake is the goal of the creation of the Ropinirole Self-NanoEmulsifying System. The solvent system for the liquid Self-NanoEmulsifying Drug Delivery System (SNEDDS) was optimized using Box-Behnken Design, where the concentration of oil(X1), surfactant (X2), and co-surfactant(X3) were taken as independent variables. The formulated liquid SNEDDS were then converted into solid SNEDDS by the adsorption method for improving patient compliance.

Results

The obtained mean droplet size of the formulated SNEDDS was 96.71 nm, and the rate of emulsification was 22 s. Liquid SNEDDS was converted into solid SNEDDS using Syloid 244 FP as adsorbent. Scanning Electron Microscopy (SEM) study shows well-separated particles adsorbed on Syloid 244 FP. In vitro drug release studies show better release from solid and liquid SNEDDS when compared to pure suspension.

Conclusions

Ropinirole-loaded SNEDDS can be a better option for reducing the extensive first-pass metabolism associated with Ropinirole.

Materials

The required pharmaceutical active ingredient Ropinirole was obtained as a gift sample from Intas Pharmaceuticals Ltd. Ahmedabad. Other excipients required for the development of SNEDDS include different oils, surfactants, and co-surfactants purchased from Chemdyes Corporation. For preliminary trials, castor oil, Capmul MCM EP, Capmul MCM C8, Miglyol 812 N, Captex 200 P, and Labrafac PG were tested for selection of appropriate oil. Similarly, Transcutol HP, Acrysol EL 135, and Acconon MC8 as co-surfactants, and Span 20, Span 80, Tween 20, and Tween 80 as surfactants were also screened. Apart from these, adsorbing agents experimented on were Aerosil 300 Pharma, Syloid 244 FP, Neusilin UFL 2, Crospovidone, and MCC for conversion of liquid SNEDDS into solid SNEDDS (Fig. 1).

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Detholia, K., Mohandas, A., Varia, U. et al. Development and optimization of Ropinirole loaded self-nanoemulsifying tablets. Futur J Pharm Sci 9, 66 (2023).
https://doi.org/10.1186/s43094-023-00516-x