Enhancement of the Solubility and Bioavailability of Pitavastatin through a Self-Nanoemulsifying Drug Delivery System (SNEDDS)

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 Cmax, Tmax, half-life, MRT, AUC, and AUMC compared to the reference formulation. Our study demonstrated that the SNEDDS effectively enhanced the solubility and bioavailability of a BCS class II drug.

Polyethylenimine‐grafted mesoporous silica nanocarriers markedly enhance the bactericidal effect of curcumin against Staphylococcus aureus biofilm

“…where μ max and μ min are the maximum and minimum mean of assay signals, and σ max and σ min are the SDs of the maximum and minimum factor is between 0.5 and 1, acceptable in some cases if it is between 0 and 0.5, and not acceptable if the Z' factor value is <0. tration of curcumin increased. 41,42 In the literature investigations, researchers have claimed the solubility of curcumin as 0.6 μg/ml in water 19 whereas in our investigations once the 0.1% (wt/vol) Tween 80 was added to HEPES buffer solution (25 mM, pH 7.2) the curcumin was solubilized 100-fold higher than the literature finding. Our observations shown in Figure 2 indicated that when curcumin loaded onto F-MSN-PEI and immersed in the 0.1% (wt/vol) Tween 80 containing HEPES buffer the solubility of curcumin improved up to 110.6 ± 5.2 μg/ml which is almost 183-fold higher 0.6 μg/ml where the solubility was investigated in water.…”

“…In this particular investigation, we have employed higher concentrations than the solubility limits, which was foreseen as the needed dosing in investigating the bactericidal effect of curcumin in the circumstance of biofilm inhibition and eradications. The observations showed that free curcumin solubility could be improved up to 58.6 ± 1.3 μg/ml and further 75.6 ± 0.4 μg/ml in 0.1% (wt/vol) Tween 80 (non‐ionic surfactant) aqueous solution once the starting concentration of curcumin increased 41,42 . In the literature investigations, researchers have claimed the solubility of curcumin as 0.6 μg/ml in water 19 whereas in our investigations once the 0.1% (wt/vol) Tween 80 was added to HEPES buffer solution (25 mM, pH 7.2) the curcumin was solubilized 100‐fold higher than the literature finding.…”

Self-Nanoemulsifying Drug Delivery System (SNEDDS) of Apremilast: In Vitro Evaluation and Pharmacokinetics Studies

“…Overall, the release profile of APR from optimized SNEDDS F9 was significant compared to the drug suspension ( p < 0.05). The noncompartmental pharmacokinetic model was used to calculate different pharmacokinetic parameters of APR including C max , AUC 0–t , AUC 0–inf , λz, T ½, T max and relative bioavailability [ 33 , 34 , 35 ]. The most significant parameters compared to the APR suspension were the T max = 4.00 ± 0.96 h, which was 2.0 ± 1.70 h for the APR suspension, AUC 0–t = 3256.76 ± 212.50 ng.h/mL compared to APR suspension 462.83 ± 52.25 ng.h/mL, AUC 0–∞ = 3481.04 ± 235.51 ng.h/mL compared to APR suspension 488.13 ± 61.31 ng.h/mL and the relative bioavailability = 703.66% compared to APR suspension = 100%, which indicated a seven-fold increase in APR bioavailability ( p ˂ 0.05).…”

Alginate as a Promising Biopolymer in Drug Delivery and Wound Healing: A Review of the State-of-the-Art

“…In NDDSs, the active carrier is a base that permits actives to be carried to the intended location, delivering the actives in a controlled manner, thereby enhancing the active bioavailability [ 12 ]. Nanoparticles, liposomes, microspheres, polymeric micelles, etc., are some of the significant actives carriers utilized in NDDSs [ 13 , 14 , 15 , 16 , 17 , 18 ].…”