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Aim:To prepare a biodegradable polymeric carrier for oral delivery of a water-insoluble drug capsaicin (CAP) and evaluate its quality.Methods:CAP-loaded methoxy poly (ethylene glycol)-poly(ε-caprolactone) nanoparticles (CAP/NPs) were prepared using a modified emulsification solvent diffusion technique. The quality of CAP/NPs were evaluated using transmission electron microscopy, powder X-ray diffraction, differential scanning calorimetry and Fourier transform infrared techniques. A dialysis method was used to analyze the in vitro release profile of CAP from the CAP/NPs. Adult male rats were orally administered CAP/NPs (35 mg/kg), and the plasma concentrations of CAP were measured with a validated HPLC method. The morphology of rat gastric mucosa was studied with HE staining.Results:CAP/NPs had an average diameter of 82.54±0.51 nm, high drug-loading capacity of 14.0%±0.13% and high stability. CAP/NPs showed a biphasic release profile in vitro: the burst release was less than 25% of the loaded drug within 12 h followed by a more sustained release for 60 h. The pharmacokinetics study showed that the mean maximum plasma concentration was observed 4 h after oral administered of CAP/NPs, and approximately 90 ng/mL of CAP was detected in serum after 36 h. The area under the curve for the CAP/NPs group was approximately 6-fold higher than that for raw CAP suspension. Histological studies showed that CAP/NPs markedly reduced CAP-caused gastric mucosa irritation.Conclusion:CAP/NPs significantly enhance the bioavailability of CAP and markedly reduce gastric mucosa irritation in rats. [ABSTRACT FROM AUTHOR]

The development, survival, reproduction, and life-span of Bemisia tabaci (Gennadius) on six major cotton varieties (Xinluzao 8, Xinluzao 16, Xinluzao 17, Zhongmian 35, Kang 5, and Dai 80) in Xinjiang were studied u nder the conditions of (26±1) °C, relative humidity (75±1)%, and illumination L :D=16:8 in laboratory. The life table of the B. tabaci e xperimental population was established, and the population net reproductive rate (R0), intrinsic rate of increase (rm), mean generation time (T) , and finite growth rate (λ) were estimated. Significant differences were o bserved in the size, development duration, survival, and fecundity of the experi mental population on the six cotton varieties. The fecundity and survival rate o f B. tabaci were the highest on Xinluzao 16 and the lowest on Kang 5. Xinluz ao 16 was the most appropriate host for the growth and development of B. tabaci population, followed by Zhongmian 35, while Kang 5 was the m ost unsuitable host. [ABSTRACT FROM AUTHOR]

Affinity chromatography is characterized by its high specificity,high recovery rate and sensitivity,and it has been widely used in the selection of active ingredients of traditional Chinese medicine,separation and enrichment of low molecular weight sugars and protein peptides,research on mechanism of action and discovery of targets.This paper reviewed the application of affinity chromatography and its adsorption isotherm model,kinetic model and adsorption thermodynamic mechanism in the field of traditional Chinese medicine.This summarizes and provides thinking for comprehensive applications of affinity chromatography theory in the field of active ingredient screening,purification and medicine interaction.

Hypolipidemic polysaccharides have notable activity and safety with a range of diverse sources. In this paper, the classification of hypolipidemic polysaccharides was carried out into polysaccharide sulfate, glycosaminoglycan, homopolysaccharide and heteropolysaccharide. The hypolipidemic activity mechanism and structure-activity relationship hypothesis of those polysaccharides in recent years were briefly reviewed therefore to provide references for the study and product development of polysaccharides., Competing Interests: The authors of this article and the planning committee members and staff have no relevant financial relationships with commercial interests to disclose., (Copyright© by the Chinese Pharmaceutical Association.)

Recent years, chemical constituents from spice volatile oils have gained worldwide concern owing to its multiple pharmacological effects and safety for using as the natural antibacterial agents. However, their poor dissolution, strong volatility, serious irritation, weak stability, easy oxidation and low bioavailability characteristics are the major obstacle in the preparation of effective oral formulation and practical application. Therefore, there is an urgent need to select a novel carrier system that can delivery the chemical constituents from spice volatile oils more efficiently with improving their stability as well as alleviating the irritation, and develop the functional food, health products and even medicine for exerting their pharmacological effects, which also is the focus and nodus of the research on their application. This review presents recent systematic studies on their novel carrier systems, including cyclodextrin inclusion complex, liposomes, nanoemulsions, nanoparticles, solid dispersion and so on, and summarizes the characteristics, application range and problems of each novel carrier systems, in order to provide some beneficial thoughts in further developing new products of chemical constituents from spice volatile oils.

Linalool, as a major volatile compound, is widely distributed in natural plant essential oil. In addition, it can also be artificially synthesized. Linalool is used frequently as an important ingredient of perfumes and household detergents. It is still employed in food flavor and industries. Besides, linalool has some positive effect on healthcare. Many studies have showed that linalool exhibited a variety of pharmacological activities, including analgesic, anxiolytic, sedative, anti-inflammatory, anti-tumor and anti-bacterial effects. Therefore, linalool will be a promising agent for clinical application. This article reviews the pharmacological effects and formulation studies of linalool so as to provide a theoretical basis for its further development and utilization.

Pluronic/bile salt/phospholipid mixed micelles (Pluronic/BS/PS-MM) drug carrier system for solubilization hydrophobic drugs was developed. A typical hydrophobic compound, pyrene, was selected as a representative hydrophobic compound to model the hydrophobic drugs. Five Pluronics, F68, F88, F98, F108, and F127 with different PPO chain length were studied. CMC data and solubilization capacities were obtained from a pyrene solubilization method. A closed association model was used to obtain the thermodynamic parameters: Gibbs free energy (ΔG°), enthalpy, (ΔH°) and entropy (ΔS°) of micellization. The results obtained from these experiments suggest that the mixed micelles was more stable and solubilize more pyrene than single one; and the solubilization of pyrene was strong effected by the PPO block size, thus accentuating synergistic interaction mechanism in Pluronic/BS/PS-MM. The study generated an important dataset so as to compare the effect of different Pluronics on solubility capacity of Pluronic/BS/PS-MM.

Background: The purpose of this study was to develop a sustained drug-release model for water-soluble drugs using silica nanoparticles., Methods: Hollow-type mesoporous silica nanoparticles (HMSNs) were prepared using Na(2)CO(3) solution as the dissolution medium for the first time. The water-soluble compound, silybin meglumine, was used as the model drug. The Wagner-Nelson method was used to calculate the in vivo absorption fraction., Results: The results of transmission electron microscopy and nitrogen adsorption revealed that the empty HMSNs had uniformly distributed particles of size 50-100 nm, a spherical appearance, a large specific surface area (385.89 ± 1.12 m(2)/g), and ultralow mean pore size (2.74 nm). The highly porous structure allowed a large drug-loading rate (58.91% ± 0.39%). In 0.08 M Na(2)CO(3) solution, silybin meglumine-loaded HMSNs could achieve highly efficacious and long-term sustained release for 72 hours in vitro. The results of in vitro-in vivo correlation revealed that HMSNs in 0.08 M Na(2)CO(3) solution had a correlation coefficient R(2) value of 0.9931, while those of artificial gastric juice and artificial intestinal juice were only 0.9287 and 0.7689, respectively., Conclusion: The findings of in vitro-in vivo correlation indicate that HMSNs together with Na(2)CO(3) solution could achieve an excellent linear relationship between in vitro dissolution and in vivo absorption for 72 hours, leading to a promising model for sustained release of water-soluble drugs.

The objective of this study was to investigate the use of cationized Pleurotus eryngii polysaccharide (CPEPS) as a nonviral gene delivery vehicle to transfer plasmid DNA encoding transforming growth factor beta-1 (pTGF-β1) into mesenchymal stem cells (MSCs) in vitro. Crude P. eryngii polysaccharide was purified, and then cationized by grafting spermine onto the backbone of the polysaccharide. Agarose gel electrophoresis, transmission electron microscopy, and a Nano Sense Zetasizer (Malvern Instruments, Malvern, UK) were used to characterize the CPEPS-pTGF-β1 nanoparticles. The findings of cytotoxicity analysis showed that when the nanoparticles were formulated with a CPEPS/pTGF-β1 weight ratio ≥ 10:1, a greater gel retardation effect was observed during agarose gel electrophoresis. The CPEPS-pTGF-β1 nanoparticles with a weight ratio of 20:1, respectively, possessed an average particle size of 80.8 nm in diameter and a zeta potential of +17.4 ± 0.1 mV. Significantly, these CPEPS-pTGF-β1 nanoparticles showed lower cytotoxicity and higher transfection efficiency than both polyethylenimine (25 kDa) (P = 0.006, Student's t-test) and Lipofectamine(TM) 2000 (P = 0.002, Student's t-test). Additionally, the messenger RNA expression level of TGF-β1 in MSCs transfected with CPEPS-pTGF-β1 nanoparticles was significantly higher than that of free plasmid DNA-transfected MSCs and slightly elevated compared with that of Lipofectamine 2000-transfected MSCs. Flow cytometry analysis demonstrated that 92.38% of MSCs were arrested in the G1 phase after being transfected with CPEPS-pTGF-β1 nanoparticles, indicating a tendency toward differentiation. In summary, the findings of this study suggest that the CPEPS-pTGF-β1 nanoparticles prepared in this work exhibited excellent transfection efficiency and low toxicity. Therefore, they could be developed into a promising nonviral vector for gene delivery in vitro.

Nanocarriers generally made of natural or artificial polymers ranging in size from about 10-1 000 nm, possess versatile properties suitable for drug delivery, including good biocompatibility and biodegradability, potential capability of targeted delivery and controlled release of incorporated drugs, and have been extensively used in the development of new drug delivery systems (DDS). These types of nano-DDS have considerable potential to traditional Chinese medicine (TCM), and recently have attracted increasing efforts on the TCM research and development. In this review, the recently published literature worldwide is covered to describe the latest advances in the applications as TCM delivery carriers, and to highlight the characteristics and preparation methods of some selected examples of promising nanocarriers such as nanoparticles, lipid nanoparticles, nanoemulsions, nanomicelles and nanoliposomes.

Objective: To prepare silybin lipid nanospheres (SLN) and to evaluate the properties of morphology, particle size and the silybin distribution in mice., Method: Silybin lipid nanospheres were prepared by thin film emulsion-high pressure homogenization technique. Concentrations of silybin in mice blood, liver, spleen, lung, kidney, brain, heart, stomach after oral administration were determined by high performance liquid chromatography., Result: Scanning electron micrograph showed that most of the SLN were spherical. The average diameter from photon correlation spectrometer was 148.9 nm with the polydispersity 0.17. Body distribution data indicated that SLN could increase the distribution of silybin in blood and liver, decrease the amount of silybin in stomach as compared with the preparation on market, and the drug targeting index (DTI) in liver was 1.81., Conclusion: SLN can increase the uptake of silybin in liver after oral administration, which must benefit the hepatitis treatment.

Objective: To determine the encapsulation efficiency of silybin liposomes., Method: After Silybin liposomes solution was separated through sphadex G-100 column, eluent collected was determined by the first derivative UV spectrometry., Result: The calibration curve of Silybin was linear in the range of 0.5-30.0 mg x L(-1) (r = 0.9998). The average recovery was 101.7%. The relative standard deviation was 1.8%. The results showed that the encapsulation efficiency ranged from 65.1%-83.0% when the drug/phospholipid ratio varied from 0.02-0.06. The concentration of SLB in liposomes prepared by optimum technique was 760.4 mg x L(-1) (n = 4)., Conclusion: The method is accurate, simple and suitable for the quality control of Silybin liposomes.