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DoE-Based Solid Self-microemulsifying Drug Delivery System (S-SMEDDS) Approach for Improving the Dissolution Properties of Raltegravir Potassium

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Abstract

Objective

Raltegravir potassium (RP) exhibits very low water solubility over the range of physiological pH (1.2, 4.5, and 6.8), which leads to poor dissolution properties and ultimately high intra- and inter-patient variabilities. The present research work aimed to prepare RP-loaded solid self-microemulsifying drug delivery system (S-SMEDDS) of RP to improve its dissolution characteristics.

Methods

Based on results of drug solubilization capacity and emulsification efficiency, labrasol, Tween-20, and PEG-400 were selected as oil, emulsifier, and co-emulsifier, respectively. A ternary phase diagram was generated to identify the proportion of compositions that, upon mixing, formed a clear and transparent microemulsion. In the present investigation, simplex lattice design was used to explore the effect of variations in the composition of excipients on significant formulation characteristics.

Result

The regression analysis suggested a significant effect of the change in the proportion of composition on selected response variables. Optimized SMEDDS formulation was mixed with selected carriers in a mortar to prepare S-SMEDDS. The results of DSC and powder X-ray diffraction studies indicated the complete transformation of the crystalline drug into the amorphous or molecular level dispersed form when neusiline US2 was used as a carrier.

Conclusion

The results of in vitro dissolution studies proved significant improvement in the dissolution properties from the S-SMEDDS formulation compared to the pure drug (f2 < 50).

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Funding

The Department of Technical Education, Government of Gujarat, India, has given financial assistance under the SSIP (Student Startup & Innovation Policy) scheme for this project.

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Authors and Affiliations

  1. B.K. Mody Government Pharmacy College, Polytechnic Campus, Near Ajidam, Rajkot, Gujarat, 360005, India

    Sourabhkumar Jain, M. M. Soniwala, Nirav Kotadiya & Dhavalkumar Mori

  2. R. K. School of Pharmacy, R.K. University, Rajkot, India

    Kiran Dudhat

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  1. Sourabhkumar Jain
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Correspondence to Dhavalkumar Mori.

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Jain, S., Dudhat, K., Soniwala, M.M. et al. DoE-Based Solid Self-microemulsifying Drug Delivery System (S-SMEDDS) Approach for Improving the Dissolution Properties of Raltegravir Potassium. J Pharm Innov 18, 29–42 (2023). https://doi.org/10.1007/s12247-022-09621-5

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