Efavirenz Loaded Mixed Polymeric Micelles: Formulation, Optimization, and In Vitro Characterization

Abstract

Efavirenz (EFZ) is a biopharmaceutics classification system (BCS) Class-II, first-line antiretroviral (ARV) drug. However, its utility through the oral route is restricted by its poor solubility. The objective of this study was to formulate EFZ-loaded binary-mixed micelles as a potential carrier for oral administration of EFZ. Rubingh's regular solution theory was used to determine the interaction behavior of the two components (Cremophor RH 40 and Phospholipon 80H) and of the mixed micelles and synergistic behavior was confirmed. The mixed miceller system was formulated using solvent evaporation method and a 3 2 factorial design was used for the optimization of selected independent variables. Miceller systems were further characterized in terms of morphology, particle size, zeta potential, percent entrapment efficiency, and drug loading. Fourier transform infrared and differential scanning calorimetry measurements confirmed the entrapment of EFZ in the micelles. The optimized formulation presented desirable qualities viz., nanometric size (17.27 -0.079), high entrapment efficiency, and good colloidal stability. The prepared optimized micelles can be potential carriers for EFZ in ARV therapies.

Curcumin-Loaded RH60/F127 Mixed Micelles: Characterization, Biopharmaceutical Characters and Anti-Inflammatory Modulation of Airway Inflammation

“…I 373nm /I 384nm is frequently used to characterize the polarity of the environment in which the pyrene probe is located, with a larger value indicating a more polar microenvironment for the flower probe and a smaller I 373nm /I 384nm indicating a less polar microenvironment. Figure 3 shows CMCs of 0.82, 0.002, and 0.004 mg/mL for F127, RH60, and RH60/F127-MMs, respectively, which are consistent with the literature [ 37 , 38 ]. Due to the large amount of RH60 in the Cur-RH60/F127-MMs (80%), the CMC of RH60/F127-MMs was biased toward RH60.…”

“…for the flower probe and a smaller I373nm/I384nm indicating a less polar microenvironment. Figure 3 shows CMCs of 0.82, 0.002, and 0.004 mg/mL for F127, RH60, and RH60/F127-MMs, respectively, which are consistent with the literature [37,38]. Due to the large amount of RH60 in the Cur-RH60/F127-MMs (80%), the CMC of RH60/F127-MMs was biased toward RH60.…”

Drug Screening, Oral Bioavailability and Regulatory Aspects: A Need for Human Organoids

“…Within the enterocytes, lipids are resynthesized and assembled into chylomicrons and high density lipoproteins for secretion [47]. The physiological pathway of fat digestion and uptake has gained increasing attention in drug development, as micelles can act as nanocarriers promoting the oral absorption of hydrophobic drugs and nutrients [21,48,49], and association of drugs with chylomicrons might prevent metabolic inactivation by avoiding the hepatic first-pass liver metabolism, as chylomicrons are transported via the lymphatic circulation [4]. Alternatively, enterocyte lipid metabolism may be targeted pharmacologically to lower systemic lipid load and energy intake, thus affecting hyperlipidemia, obesity, metabolic syndrome, steatosis, insulin resistance, atherosclerosis and other disorders [5,47].…”

Tunable Polymeric Mixed Micellar Nanoassemblies of Lutrol F127/Gelucire 44/14 for Oral Delivery of Praziquantel: A Promising Nanovector against Hymenolepis nana in Experimentally-Infected Rats

“…PMMs are kinetically stable nanosystems tailored via the self-assembly of amphiphilic entities in water, beyond critical micelle concentration (CMC), into a core-shell architecture. The inner core constitutes the hydrophobic portion of the PMMs embedding lipophilic drugs such as PRZ, whereas the hydrophilic corona surmounts drug inactivation by biological milieu like the GIT [ 15 ]. A representative of these polymers is Lutrol block copolymers, which are versatile amphiphilic polymers composed of hydrophobic poly(propylene oxide) (PPO) as a central block flanked by two hydrophilic poly(ethylene oxide) (PEO) blocks basically constructed into a triblock array: PEO–PPO–PEO.…”

“…Intriguingly, the prospective exploitation of PMMs as oral nano-cargos was verified through promoted bioavailability and pharmacodynamics of various drugs encompassing valsartan [ 20 ], efavirenz [ 15 ] and icaritin [ 16 ], owing to their unique and inherent characteristics such as controllable and minute size (<100 nm), sustained release of the laden drugs, along with superior hydrosolubility and intestinal permeability. According to the preceding remarks, we hypothesized that PRZ-PMMs could enhance the bioavailability/cellular delivery, conquer the rapid clearance, upgrade the dosage proportionality and minimize the inter-patient variability, thus lowering the overall recommended dose to be orally delivered.…”