Ethanol injection method for hydrophilic and lipophilic drug-loaded liposome preparation

Jaafar‐Maalej, Chiraz; Diab, Roudayna; Andrieu, Véronique; Elaı̈ssari, Abdelhamid; Fessi, Hatem

doi:10.3109/08982100903347923

Cited by 290 publications

(186 citation statements)

References 57 publications

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“…Previous studies demonstrated that increase in lipophilic character (log P) also resulted in an increased EE due to the higher affinity of drug molecules to the lipids inside the bilayer structure. [29][30][31] Moreover, an EE .90% for CoQ10 was achieved by other studies with comparable results. 32,33 Ps, PdI, ZP and morphology PS, PdI and ZP measurements were conducted for all liposomal formulations prepared for studying the experimental design.…”

Section: Optimization Studysupporting

confidence: 69%

Design, optimization and characterization of coenzyme Q10- and D-panthenyl triacetate-loaded liposomes

Çelik¹,

Sagiroglu²,

Özdemir³

2017

IJN

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Coenzyme Q10 (CoQ10) is a lipid-soluble molecule found naturally in many eukaryotic cells and is essential for electron transport chain and energy generation in mitochondria. D-Panthenyl triacetate (PTA) is an oil-soluble derivative of D-panthenol, which is essential for coenzyme A synthesis in the epithelium. Liposomal formulations that encapsulate both ingredients were prepared and optimized by applying response surface methodology for increased stability and skin penetration. The optimum formulation comprised 4.17 mg CoQ10, 4.22 mg PTA and 13.95 mg cholesterol per 100 mg of soy phosphatidylcholine. The encapsulation efficiency of the optimized formulation for CoQ10 and PTA was found to be 90.89%±3.61% and 87.84%±4.61%, respectively. Narrow size distribution was achieved with an average size of 161.6±3.6 nm, while a spherical and uniform shape was confirmed via scanning electron microscopy and transmission electron microscopy images. Cumulative release of 90.93% for PTA and 24.41% for CoQ10 was achieved after 24 hours of in vitro release study in sink conditions. Physical stability tests indicated that the optimized liposomes were suitable for storage at 4°C for at least 60 days. The results suggest that the optimized liposomal formulation would be a promising delivery system for both ingredients in various topical applications.

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Section: Optimization Studysupporting

confidence: 69%

Design, optimization and characterization of coenzyme Q10- and D-panthenyl triacetate-loaded liposomes

Çelik¹,

Sagiroglu²,

Özdemir³

2017

IJN

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“…It was previously found that the particle size in membrane-based particle fabrication processes was smaller at the higher wall shear stress, 24,31 which was associated with higher mixing efficiency. 32,33 Thus, high homogenous supersaturation may occur in a short time, leading to rapid self-arrangement of polymers and formation of small micelles. Our results suggest that for a given set of conditions, an agitator speed of 700 rpm was the optimal speed, since the produced micelles were both relatively uniform and of suitable size.…”

Section: Resultsmentioning

confidence: 99%

pH-Sensitive Micelles for Targeted Drug Delivery Prepared Using a Novel Membrane Contactor Method

Laouini

Koutroumanis

Charcosset

et al. 2013

ACS Appl. Mater. Interfaces

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A novel membrane contactor method was used to produce size-controlled poly(ethylene glycol)-b-polycaprolactone (PEG-PCL) copolymer micelles composed of diblock copolymers with different average molecular weights, M n (9200 or 10 400 Da) and hydrophilic fractions, f (0.67 or 0.59). By injecting 570 L m −2 h −1 of the organic phase (a 1 mg mL −1 solution of PEG-PCL in tetrahydrofuran) through a microengineered nickel membrane with a hexagonal pore array and 200 μm pore spacing into deionized water agitated at 700 rpm, the micelle size linearly increased from 92 nm for a 5-μm pore size to 165 nm for a 40-μm pore size. The micelle size was finely tuned by the agitation rate, transmembrane flux and aqueous to organic phase ratio. An encapsulation efficiency of 89% and a drug loading of ∼75% (w/w) were achieved when a hydrophobic drug (vitamin E) was entrapped within the micelles, as determined by ultracentrifugation method. The drug-loaded micelles had a mean size of 146 ± 7 nm, a polydispersity index of 0.09 ± 0.01, and a ζ potential of −19.5 ± 0.2 mV. When drug-loaded micelles where stored for 50 h, a pH sensitive drug release was achieved and a maximum amount of vitamin E (23%) was released at the pH of 1.9. When a pH-sensitive hydrazone bond was incorporated between PEG and PCL blocks, no significant change in micelle size was observed at the same micellization conditions.

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“…Variable B has the second largest effect on response value Y. 31 Comparing areas of Y value more than 7.5 in contour plots for Y, variable B and C have a small variable range at a fixed level of variable A (Figure 1D-F). It was also confirmed that variable A is the main factor.…”

Section: Optimization Of Formulation For Irak/abt-npmentioning

confidence: 99%

Cooperation of IRAK1/4 inhibitor and ABT-737 in nanoparticles for synergistic therapy of T cell acute lymphoblastic leukemia

Wu¹,

Wang²,

Qiu³

et al. 2017

IJN

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T cell acute lymphoblastic leukemia (T-ALL) is caused by clonal expansion of variant T cell progenitors and is considered as a high risk leukemia. Contemporary single chemotherapy has a limited effect due to dynamic and versatile properties of T-ALL. Here IRAK1/4 inhibitor and ABT-737 were co-encapsulated into polyethylene glycol modified poly (lactic-co-glycolic acid) nanoparticles (IRAK/ABT-NP) to enhance synergistic therapy of T-ALL. The formulation was optimized to achieve high drug loading using Box-Behnken design and response surface methodology. The optimal parameter comprised 2.98% polymer in acetonitrile, a ratio of oil phase to water phase of 1:8.33, and 2.12% emulsifier concentration. High drug loading and uniform spherical shape was achieved. In vitro release study showed sustained release of IRAK1/4 inhibitor for 72 hours as well as sustained release of ABT-737 for more than 120 hours. Uptake efficiency of IRAK/ABT-NP and induced apoptotic T-ALL fraction by IRAK/ABT-NP were much higher than the IRAK1/4 and ABT-737 combined solution. IC 50 of IRAK/ABT-NP was two-fold lower than free drug combination in Jurkat cells. Additionally, we conducted in vivo experiments in which IRAK/ABT-NP exhibited greater cytotoxicity toward T-ALL cells, the capacity to significantly restore white blood cell number in peripheral blood, and improved survival time of T-ALL mouse model compared to the IRAK1/4 and ABT-737 combined solution.

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Ethanol injection method for hydrophilic and lipophilic drug-loaded liposome preparation

Cited by 290 publications

References 57 publications

Design, optimization and characterization of coenzyme Q10- and D-panthenyl triacetate-loaded liposomes

Design, optimization and characterization of coenzyme Q10- and D-panthenyl triacetate-loaded liposomes

pH-Sensitive Micelles for Targeted Drug Delivery Prepared Using a Novel Membrane Contactor Method

Cooperation of IRAK1/4 inhibitor and ABT-737 in nanoparticles for synergistic therapy of T cell acute lymphoblastic leukemia

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