Enhancement of the Solubility and Bioavailability of Pitavastatin through a Self-Nanoemulsifying Drug Delivery System (SNEDDS).
Title: | Enhancement of the Solubility and Bioavailability of Pitavastatin through a Self-Nanoemulsifying Drug Delivery System (SNEDDS). |
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Authors: | Ashfaq, Mehran, Shah, Shahid, Rasul, Akhtar, Hanif, Muhammad, Khan, Hafeez Ullah, Khames, Ahmed, Abdelgawad, Mohamed A., Ghoneim, Mohammed M., Ali, Muhammad Yasir, Abourehab, Mohammad A. S., Maheen, Safirah, Iqbal, Omeira, Abbas, Ghulam, El Sisi, Amani M. |
Source: | Pharmaceutics; Mar2022, Vol. 14 Issue 3, p482, 18p |
Subject Terms: | DRUG solubility, DRUG delivery systems, PITAVASTATIN, SOLUBILITY, EMULSIONS (Pharmacy), BIOAVAILABILITY, ZETA potential, PHASE diagrams |
Abstract: | The purpose of the study was to develop an SNEDDS to improve the solubility and bioavailability of pitavastatin. The solubility of pitavastatin in different oils, surfactants, and co-surfactants was determined and a pseudo-ternary phase diagram was constructed. The SNEDDS was characterized by zeta-sizer, zeta-potential, FTIR, DSC, and TGA. Release and permeation of pitavastatin from the SNEDDS was studied for 12 and 24 h, respectively. The lipolysis test, RBC lysis, effect on lipid profile, and pharmacokinetics were studied. The SPC3 formulation showed a 104 ± 1.50 nm particle size, a 0.198 polydispersity index (PDI), and a –29 zeta potential. FTIR, DSC, and TGA showed the chemical compatibility and thermal stability. The release and permeation of pitavastatin from SPC3 was 88.5 ± 2.5% and 96%, respectively. In the lipolysis test, the digestion of SPC3 yielded a high amount of pitavastatin and showed little RBC lysis. The lipid profile suggested that after 35 days of administration of the SNEDDS, there was a marked decrease in TC, LDL, and triglyceride levels. The SNEDDS of SPC3 showed an 86% viability of Caco-2 cells. Pharmacokinetics of SPC3 showed improved values of C |
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Database: | Complementary Index |
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