Preparation of PLGA nanoparticles using TPGS in the spontaneous emulsification solvent diffusion method

2007 ◽  
Vol 2 (3) ◽  
pp. 183-192 ◽  
Author(s):  
Farnaz Esmaeili ◽  
Fatemeh Atyabi ◽  
Rassoul Dinarvand
2018 ◽  
Vol 14 (5) ◽  
pp. 448-453 ◽  
Author(s):  
Shadabul Haque ◽  
Ben J. Boyd ◽  
Michelle P. McIntosh ◽  
Colin W. Pouton ◽  
Lisa M. Kaminskas ◽  
...  

Background: Poly(d,l-lactide-co-glycolide) (PLGA) based biodegradable nanoparticles are of key interest for the development of controlled release drug delivery systems and for other biomedical applications. It has been reported that PLGA polymers can be converted into colloidal nanoparticulate systems by various techniques, such as emulsification-diffusion, emulsificationevaporation, interfacial deposition, salting out, dialysis and nanoprecipitation. Emulsificationevaporation with water immiscible solvents including dichloromethane and chloroform has been the preferred method for the synthesis of PLGA nanoparticles due to the low boiling point and limited water solubility of these solvents. We and others, however, have found that when water-immiscible solvents are used for the synthesis of PLGA nanoparticles, particle aggregation, non-uniform particle size and multimodal size distribution are commonly encountered problems. This suggests that the synthesis of PLGA nanoparticles using water immiscible solvents is highly sensitive to small procedural variations that affect overall reproducibility. Objective: This study presents a simple and robust procedure for the preparation of PLGA nanoparticles with very small batch to batch variability (<5% variability in size (z-average) as determined by dynamic light scattering). Results: The results showed that the emulsification solvent diffusion method teamed with partially water-miscible solvents, such as ethyl acetate, is a versatile approach for the preparation of PLGA nanoparticles with highly reproducible sizes (between 50 and 400 nm) and zeta potentials (between - 30 and +30 mV), with relatively narrow polydispersity. Conclusion: Emulsification-diffusion with ethyl acetate is, therefore, a more reliable alternative to several existing procedures for the reproducible and refined synthesis of PLGA nanoparticles.


2015 ◽  
Vol 33 ◽  
pp. 60-71 ◽  
Author(s):  
Praewpun Boonyasirisri ◽  
Ubonthip Nimmannit ◽  
Pranee Rojsitthisak ◽  
Settapon Bhunchu ◽  
Pornchai Rojsitthisak

Curcuminoids are a mixture of phenolic compounds isolated from Curcuma longa L. (turmeric) rhizomes that possess antioxidant, anti-inflammatory, anti-Alzheimer and anticancer activities. However, curcuminoids have poor solubility in acid and neutral solutions, rapid decomposition in neutral and alkaline solutions, and low bioavailability that limits their use as therapeutic agents. To overcome these problems, statistical design for preparation and characterization of poly(D,L-lactide-co-glycolide) (PLGA) nanoparticles as a carrier for curcuminoids was evaluated in this study. The curcuminoid-loaded PLGA nanoparticles were prepared by a modified spontaneous emulsification solvent diffusion method using polyvinyl alcohol (PVA) as a stabilizer. The formulations were optimized using three-factor, three-level Box-Behnken experimental design. The independent variables in the formulations were the lactide/glycolide (LA/GA) molar ratio of PLGA (50:50 to 85:15), the curcuminoid concentration (2%-10%, w/v), and the PVA concentration (3%-7%, w/v). The dependent variables were particle size, loading capacity and entrapment efficiency. Statistical evaluation showed that the LA/GA molar ratio of PLGA and the curcuminoid and PVA concentrations all affected the characteristics of the PLGA nanoparticles. To achieve a minimum particle size and maximum loading capacity and entrapment efficiency, the optimal formulation of the curcuminoid-loaded PLGA nanoparticles had a LA/GA molar ratio of PLGA of 50:50, 10% (w/v) curcuminoids, and 3% (w/v) PVA. A sustainable in vitro release profile of curcuminoids was obtained from this optimal formulation.


2021 ◽  
Author(s):  
Dehao Fu ◽  
Yuanyuan Guo ◽  
Yongwei Liu ◽  
Chen Shi ◽  
Tingting Wu ◽  
...  

Abstract BackgroundOsteoporosis (OP) is a systemic skeletal disease marked by bone mass reduction and bone tissue destruction. Hormone replacement therapy is an effective treatment for post-menopausal OP, but estrogen has poor tissue selectivity and severe side effects.ResultsIn this study, we constructed a poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs)-based drug delivery system to co-load 17β estradiol (E2) and iron oxide (Fe3O4) together, modified with alendronate (AL) to achieve bone targeting and realize a magnetically remote-controllable drug release. The NPs were fabricated through the emulsion solvent diffusion method. The particle size was approximately 200 nm while the encapsulation efficiency of E2 was 58.34 ± 9.21%. The NPs were found to be spherical with a homogenous distribution of particle size. The NPs showed good stability, good biocompatibility, high encapsulation ability of E2 and excellent magnetic properties. The NPs could be effectively taken up by Raw 264.7 cells and were effective in enriching drugs in bone tissue. The co-loaded NPs exposed to an external magnetic field ameliorated OVX-induced bone loss through increased BV/TV, decreased Tb.N and Tb.Sp, improved bone strength, increased PINP and OC, and downregulated CTX and TRAP-5b. The haematological index and histopathological analyses displayed the NPs had less side effects on non-skeletal tissues.ConclusionsThis study presented a remote-controlled release system based on bone-targeted multifunctional NPs and a new potential approach to bone-targeted therapy of OP.


2008 ◽  
Vol 61 (2) ◽  
pp. 132-137 ◽  
Author(s):  
Hong Yuan ◽  
Ling-Fei Huang ◽  
Yong-Zhong Du ◽  
Xiao-Ying Ying ◽  
Jian You ◽  
...  

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