Humid Heat Autoclaving of Hybrid Nanoparticles Achieved by Decreased Nanoparticle Concentration and Improved Nanoparticle Stability Using Medium Chain Triglycerides as a Modifier

Gou, Jingxin; Chao, Yanhui; Liang, Yongye; Zhang, Ning; He, Haibing; Yin, Tian; Zhang, Yu; Xu, Huaizhe; Tang, Xing

doi:10.1007/s11095-016-1952-y

Cited by 9 publications

(7 citation statements)

References 39 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The solubility data shows that all of these oils could meet the DL requirements of 2.0 mg/mL. S SO , S MCT , S (MCT:SO 1:9) , S (MCT:SO 1:1) , and S (MCT:SO 9:1) were found to be 30.26 ± 0.32 mg/mL, 166.83 ± 12.86 mg/mL, 166.86 ± 35.51 mg/mL, 146.22 ± 15.67 mg/mL, and 173.21 ± 15.13 mg/mL, respectively, confirming previous reports that MCT could improve DL (Gou et al., 2016 ). In addition, MCT could modulate the stability of lipid membranes and their resistance to peroxidation (Anez-Bustillos et al., 2016 ; Luo et al., 2019 ).…”

Section: Resultssupporting

confidence: 88%

Optimization, and in vitro and in vivo evaluation of etomidate intravenous lipid emulsion

Geng

Wang

et al. 2021

Drug Delivery

View full text Add to dashboard Cite

The aim of this investigation was to develop an etomidate intravenous lipid emulsion (ETM-ILE) and evaluate its properties in vitro and in vivo . Etomidate (ETM) is a hydrophobic drug, and organic solvents must be added to an etomidate injectable solution (ETM-SOL) to aid dissolution, that causes various adverse reactions on injection. Lipid emulsions are a novel drug formulation that can improve drug loading and reduce adverse reactions. ETM-ILE was prepared using high-pressure homogenization. Univariate experiments were performed to select key conditions and variables. The proportion of oil, egg lecithin, and poloxamer 188 (F68) served as variables for the optimization of the ETM-ILE formulation by central composite design response surface methodology. The optimized formulation had the following characteristics: particle size, 168.0 ± 0.3 nm; polydispersity index, 0.108 ± 0.028; zeta potential, −36.4 ± 0.2 mV; drug loading, 2.00 ± 0.01 mg/mL; encapsulation efficiency, 97.65% ± 0.16%; osmotic pressure, 292 ± 2 mOsmol/kg and pH value, 7.63 ± 0.07. Transmission electron microscopy images showed that the particles were spherical or spheroidal, with a diameter of approximately 200 nm. The stability study suggested that ETM-ILE could store at 4 ± 2 °C or 25 ± 2 °C for 12 months. Safety tests showed that ETM-ILE did not cause hemolysis or serious vascular irritation. The results of the pharmacokinetic study found that ETM-ILE was bioequivalent to ETM-SOL. However, a higher concentration of ETM was attained in the liver, spleen, and lungs after administration of ETM-ILE than after administration of ETM-SOL. This study found that ETM-ILE had great potential for clinical applications.

show abstract

Section: Resultssupporting

confidence: 88%

Optimization, and in vitro and in vivo evaluation of etomidate intravenous lipid emulsion

Geng

Wang

et al. 2021

Drug Delivery

View full text Add to dashboard Cite

show abstract

“…Phase separation is a common phenomenon that occurs when different nonmiscible substances are blended. According to our previous studies, 17,27 lipids with shorter hydrocarbon chains are more compatible with PCL than the SL used in this study, and thus a higher lipid ratio needs to be reached before phase separation occurs. In this case, due to the stronger intermolecular forces between the long hydrocarbon chains of SL molecules, the SL was found to induce phase separation at relatively lower SL-PCL ratios (Figure 1, Figure 2, B3).…”

Section: Discussionmentioning

confidence: 99%

“…It has previously been reported that block copolymers in lipid− PCL mixed nanoparticles with nonhomogeneous cores exhibit better chemical stability in aqueous medium. 27 In this study, incorporation of SL also exhibited a block copolymer stabilizing effect, and the reason for this stabilizing effect was attributed to a decreased core polarity induced by incorporation of SL. As shown in Scheme 1A, there is less accessibility of H + or enzymes into the deeper regions of the core in SL10%-NPs, whereas the chance of H + or enzyme infiltration into the core of NPs is higher due to their higher core polarity.…”

Section: Discussionmentioning

confidence: 99%

“…Thus, the amount of SL incorporated should be precisely controlled in order to prepare nanoparticles with uniform size distributions, like SL5%-NPs and SL10%-NPs (Figure A). It has previously been reported that block copolymers in lipid–PCL mixed nanoparticles with nonhomogeneous cores exhibit better chemical stability in aqueous medium . In this study, incorporation of SL also exhibited a block copolymer stabilizing effect, and the reason for this stabilizing effect was attributed to a decreased core polarity induced by incorporation of SL.…”

Section: Discussionmentioning

confidence: 99%

“…mPEG 5k - b -PCL 14k block copolymer was synthesized by ring-opening polymerization according to the method reported previously , using mPEG 5k -OH as the initiator. Dialysis membranes (MWCO: 3.5 kDa and 14 kDa) were purchased from Ruidahenghui Co., Ltd., Beijing, China.…”

Section: Methodsmentioning

confidence: 99%

See 2 more Smart Citations

Polyester–Solid Lipid Mixed Nanoparticles with Improved Stability in Gastro-Intestinal Tract Facilitated Oral Delivery of Larotaxel

et al. 2017

Self Cite

View full text Add to dashboard Cite

The objective of this study was to investigate the role of core stability of nanoparticles on their performances in oral drug delivery. Solid lipids (Geleol Mono and Diglycerides Nf) were incorporated into nanoparticles composed of mPEG-b-PCL by the dialysis method. The prepared solid lipid loaded nanoparticles were found to be spherical nanoparticles with a core state and size distribution dependent on the amount of solid lipid incorporated. The critical aggregation concentrations of lipid-loaded nanoparticles were determined using pyrene fluorescence. Then, the stability of block copolymer in nanoparticles with different solid lipid contents was studied in simulated gastric fluid and simulated intestinal fluid. Solid lipids were found to stabilize nanoparticle cores by improving not only the thermodynamic stability (lowered CAC) of the nanoparticle but also the chemical stability of the block copolymer in the gastrointestinal environment. The stability of the loaded drug (larotaxel, LTX) in nanoparticles with different solid lipid contents was challenged by intestinal homogenate and rat liver microsome, and solid lipid loaded nanoparticles showed superior drug-protecting capability. Solid lipid incorporation exhibited limited influence on the cytotoxicity and cellular uptake but improved the transcytosis of nanoparticles in Caco-2 monolayers. The results of pharmacokinetic study indicated that core stabilization was helpful in promoting oral larotaxel absorption as the absolute bioavailability of LTX delivered by solid lipid loaded nanoparticles was found to be 13.17%, compared with that by the lipid-free nanoparticles (6.264%) and LTX solution (2.435%). Additionally, the results of biodistribution study indicated relatively higher particle integrity of solid lipid loaded nanoparticles, shown by slower liver and spleen accumulation rate, compared with its lipid-free counterpart. Overall, incorporation of solid lipids made the nanoparticles more suitable for oral drug delivery.

show abstract

Biodegradable Polymersomes as Nanocarriers for Doxorubicin Hydrochloride: Enhanced Cytotoxicity in MCF-7/ADR Cells and Prolonged Blood Circulation

et al. 2016

View full text Add to dashboard Cite

show abstract

Humid Heat Autoclaving of Hybrid Nanoparticles Achieved by Decreased Nanoparticle Concentration and Improved Nanoparticle Stability Using Medium Chain Triglycerides as a Modifier

Abstract: Incorporation of high amount of MCT changed the morphology of PEG-b-PCL based nanoparticles to an emulsion-like structure and the nanoparticles prepared could withstand autoclaving due to improved particle stability and decreased particle concentration caused by MCT incorporation.

Cited by 9 publications

References 39 publications

Optimization, and in vitro and in vivo evaluation of etomidate intravenous lipid emulsion

Optimization, and in vitro and in vivo evaluation of etomidate intravenous lipid emulsion

Polyester–Solid Lipid Mixed Nanoparticles with Improved Stability in Gastro-Intestinal Tract Facilitated Oral Delivery of Larotaxel

Biodegradable Polymersomes as Nanocarriers for Doxorubicin Hydrochloride: Enhanced Cytotoxicity in MCF-7/ADR Cells and Prolonged Blood Circulation

Contact Info

Product

Resources

About