ABSTRACT
Background: The study was aimed to prepare and evaluate tamoxifen loaded controlled release liposomes to reduce the side effects of tamoxifen during cancer treatment. Methods: Different tamoxifen loaded liposomes were prepared by modified ether injection (MEIM) and thin film hydration method (TFHM) under prescribed conditions. The prepared liposomes were characterized by using optical microscopy, evaluating encapsulation efficiency, in-vitro and ex-vivo diffusion studies by using dialysis membrane and chicken intestinal sac respectively.Results: The data revealed that all of the liposomes were spherical in shape and stable under three physical conditions i.e. 4, 25 and 37 ± 2°C temperatures and 60 ±5% relative humidity. Additionally most of the liposomes followed zero order and class II release kinetics. It was also observed that with the increase of phospholipids and cholesterol, entrapment efficiency of liposome vesicles increased thus giving a controlled release drug delivery system but further increase reduced this efficiency at a certain level.Conclusion: The formulated control release liposomes might be a good drug delivery system for target oriented drug delivery with minimum side effects of tamoxifen during cancer treatment
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Objective: To prepare pegylated long-circulating liposomes co-encapsulated by costunolide (Cos) and dehydrocostus lactone (DL), optimize the formulation and process, and evaluate the quality. Methods: The pegylated long-circulating liposomes co-encapsulated by Cos and DL were prepared by film hydration method. Single factor test and Box-Behnken response surface methodology were used to optimize the preparation process with encapsulation efficiency of Cos and DL as the index. The particle size, surface potential, encapsulation efficiency and in vitro release of the liposomes were evaluated. Results: The optimal preparation conditions were as follows: drug-to-lipid ratio was 0.14, ratio of cholesterol to phospholipid was 0.05, mPEG-2000-DSPE addition amount was 6%, hydration time was 30 min, and probe ultrasonic time was 4 min. The obtained liposome was round and uniform in distribution, with an average particle size of (104.8 ± 2.48) nm, a polydispersity index (PDI) of (0.245 ± 0.031), and a Zeta potential of (-9.7 ± 0.23) mV, the encapsulation efficiency of Cos and DL were (91.9 ± 2.6)% and (94.41 ± 1.23)%, respectively. Conclusion: The PEGylated long-circulating liposome prepared by the process and prescription optimization has good appearance and high encapsulation efficiency, which can meet the application requirements.
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Objective: To optimize the formula and preparation process of docetaxel-loaded pluronic P123 micelles. Methods:Docetaxel-loaded pluronic P123 micelles were prepared by a thin-film hydration method and optimized by central composite design and response surface methodology. The influencing factors including the quantity of docetaxel, volume of organic phase, volume of hydra-tion and temperature of hydration were investigated with the entrapment efficiency as the index. The morphology of micelles was ob-served under a transmission electron microscope. The particle diameter and zeta potential were determined. The in vitro release property was measured by a dialysis method. Results:The relationship between the influencing factors and the evaluation parameter was fitted by multi-linear equation, quadratic polynomial equation and cubic polynomial equation, respectively. The results showed that the cubic polynomial equation was superior to the others according to the correlation coefficient. Docetaxel-loaded pluronic P123 micelles were spherical with the mean diameter, zeta potential, polydispersity index, encapsulation efficiency and drug loading of 108. 3 nm,-3. 99 mV, 0. 265, (97. 91 ± 0. 28)% and (3. 72 ± 0. 12)%, respectively. The cumulative release in vitro reached 95. 03% in 120 h, and docetaxel-loaded pluronic P123 micelles had notable sustained-release property. Conclusion: The technical process for do-cetaxel-loaded pluronic P123 micelles is simple and usable, and docetaxel-loaded pluronic P123 micelles show high encapsulation effi-ciency and notable sustained-release property.
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To improve the solubility and antitumor activity of ampelopsin, ampelopsin-loaded nanomicelles from the mixture of pluronic F127 and D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS1000) were prepared by film-thin hydration method, in order to optimize the process conditions and physicochemical properties. The antitumor activities against MCF-7 cells between ampelopsin and nanomicelles were compared by MTT method, respectively. The results showed that the optimal nanomicelles were round with the nanometric size of (22.6±0.5) nm, encapsulation efficiency rate of (80.42±1.13)%, and drug-loading rate of (4.41±0.26)%. The solubility of ampelopsin in mixed nanomicelles significantly increased by 16 times. In different release media, the mixed nanomicelles could release more than 90% of drug in 8 h, and showed stronger cytotoxicity and inhibition against MCF-7 cells (P<0.01). The mixed nanomicelles can be used as new drug delivery system of ampelopsin.
ABSTRACT
Objective: To prepare baicalin-loaded TPGS nanomicells (BCN-TPGS-PMs) and to evaluate its physicochemical properties, in vitro release behavior, and antitumor activity against MCF-7 cells. Methods: BCN-TPGS-PMs were prepared by film-thin hydration method. The preparation methods and formulations were optimized and screened based on particle size and encapsulation efficiency (EE) of micelles. The transmission electron microscope (TEM) was used to observe the particle appearance, zetasizer instrument was used to detect the diameter and Zeta potential, and ultracentrifugation was utilized to determine the EE and drug-loading rate. Dynamic dialysis method was used to study the in vitro release behavior of BCN-TPGS-PMs, and the antitumor activity against MCF-7 cells was determined by MTT method. Results: The optimal BCN-TPGS-PMs were round with the nanometric size of (11.91 ± 0.14) nm, high EE rate of (95.83 ± 7.34)%, and drug-loading rate of (5.42 ± 0.04)%. The in vitro release behavior showed that BCN-TPGS-PMs had a slow release. Compared with free BCN, BCN-TPGS-PMs showed stronger cytotoxicity and inhibition against MCF-7 cells (P < 0.05). Conclusion: The prepared BCN-TPGS-PMs have small particle size, high drug-loading rate, and good stability, and could obviously increase the in vitro inhibitory effect of BCN.