Solid self Nano-Emulsifying system for the enhancement of dissolution and bioavailability of prasugrel HCl: in vitro and in vivo study

Prasugrel Hydrochloride (PHCl) is an antiplatelet drug. It is a class II drug with variable bioavailability. The objective of this work was to enhance the solubility and hence the bioavailability and efficacy of PHCl. A Self Nano-Emulsifying Drug Delivery System (SNEDDS) was prepared using Kolliphor El, Maisine 35-1, and Transcutol P as surfactant, oil, and co-surfactant, respectively in a ratio 10:72:18 v/v%. The SNEDDS was converted into solid by adsorption onto Neusilin. In vitro release of the drug from SNEDDS in (pH =4) at 37 °C and 75 rpm for 45 minutes was studied.

The results were compared to those from the unprocessed PHCl and Lexar® (the commercial drug). In-vivo studies (platelet Aggregation and bleeding time) were conducted using rats as animal models. It was found that the particle size of the SNEDDS ranged between 80 and 155 nm and. EE% was 90.2% ± 0.4. The release from SNEDDS was about 84% compared to around 25% from unprocessed PHCl and 65% from Lexar^® after 15 min. The platelet aggregation of the formula was lower than the PHCl, and Lexar^® indicating higher bioavailability. In conclusion SNEDDS with high EE% was prepared and was successful in enhancing the solubility, dissolution rate and the bioavailability.

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Mai Khanfar, Suhair Al-Nimry & Shatha Attar (2021) Solid self Nano-Emulsifying system for the enhancement of dissolution and bioavailability of prasugrel HCl: in vitro and in vivo study, Pharmaceutical Development and Technology, DOI: 10.1080/10837450.2021.1973495