Separation, characterization and anti-psoriasis effect of self-assembled nanoparticles from Shaoyao Gancao Decoction / 中国中药杂志

This study aims to separate and characterize self-assembled nanoparticles(SAN) from Shaoyao Gancao Decoction(SGD) and determine the content of active compounds. Further, we aimed to observe the therapeutic effect of SGD-SAN on imiquimod-induced psoriasis in mice. The separation of SGD was performed by dialysis, and the separation process was optimized by single factor experiment. The SGD-SAN isolated under the optimal process was characterized, and the content of gallic acid, albiflorin, paeoniflorin, liquiritin, isoliquiritin apioside, isoliquiritin, and glycyrrhizic acid in each part of SGD was determined by HPLC. In the animal experiment, mice were assigned into a normal group, a model group, a methotrexate group(0.001 g·kg~(-1)), and SGD, SGD sediment, SGD dialysate, and SGD-SAN groups of different doses(1, 2, and 4 g·kg~(-1)) respectively. The psoriasis grade of mice was evaluated based on the pathological changes of skin lesions, the content of inflammatory cytokines, organ index and other indicators. The results showed that SAN obtained by centrifugation at 13 000 r·min~(-1) for 30 min was stable after dialysis for 4 times, which were uniform spherical nanoparticles with the particle size of(164.43±1.34) nm, the polydispersity index of(0.28±0.05), and the Zeta potential of(-12.35±0.80) mV. The active compound content accounted for more than 70% of SGD. Compared with the model group, SAN and SGD decreased the skin lesion score, spleen index, and inflammatory cytokine levels(P<0.05 or P<0.01) and alleviated the skin thickening and infiltration of inflammatory cells. However, the sediment group and the dialysate group had no obvious effect. SGD showed a good therapeutic effect on imiquimod-induced psoriasis in mice, and SAN demonstrated the effect equivalent to SGD in a dose-dependent manner. Therefore, we conclude that the SAN formed during decocting is the main active form of SGD, which can lower the levels of inflammatory cytokines, promote the normal differentiation of keratinocytes, and reduce the infiltration of inflammatory cells in the treatment of psoriasis lesions in mice.

Effects of self-assembled nanoparticles from Shaoyao gancao decoction on the in vitro release and intestinal absorption of the main components of Glycyrrhiza uralensis / 中国药房

OBJECTIVE To study the effects of self-assembled nanoparticles from Shaoy ao gancao decoction （SGD-SAN）on the in vitro release and intestinal absorption of the main components of Glycyrrhiza uralensis . METHODS Gancao single decoction （GSD），Shaoyao single decoction （SSD），mixed suspension of Shaoyao and Gancao single decoction （MSSGD）and SGD （i.e. Shaoyao-Gancao decoction ）were prepared ，and SAN was characterized. HPLC method was adopted to determine the contents of 7 main components （liquiritin apioside ， liquiritin， isoliquiritin apioside ， isoliquiritin， liquiritigenin， glycyrrhizic acid ， isoliquiritigenin）in G. uralensis . The dialysis bag method was used to investigate the effects of the formation of SGD-SAN on in vitro release of 7 main components in G. uralensis with pH 1.2 HCl solution and pH 6.8 phosphate buffered solution （PBS）as release media. Single-pass intestinal perfusion study was performed to investigate the effects of the formation of SGD-SAN on the intestinal absorption of 7 main components from G. uralensis . RESULTS SAN with particle size of 200-300 nm and polydispersity index of 0.3-0.5 was found in GSD ，MSSGD and SGD. GSD-SAN and MSSGD-SAN were in rod shape while SGD-SAN was irregularly spherical under transmission electron microscope. The results of in vitro release study showed that the formation of SGD-SAN could significantly increase in vitro release of liquiritigenin ，isoliquiritigenin and glycyrrhizic acid ，and had no effect on other components of G. uralensis in pH 1.2 HCl solution. The formation of SGD-SAN also had no effect on the release of each component from G. uralensis in pH 6.8 PBS. The results of intestinal perfusion experiments showed that the formation of SGD-SAN could significantly promote the absorption of each component from G. uralensis in the ileum. CONCLUSIONS- The formation of SGD-SAN significantly improves the in vitro release of poorly soluble components from G. uralensis and promotes the intestinal absorption of main components from G. uralensis ，which is the physical structure basis for the compatibility and synergy of Paeonia lactiflora and G. uralensis .

Advances in formation and application of self-assembled nanoparticles from traditional Chinese medicine / 中国中药杂志

Due to the diverse sources and unique structures, the chemical components of Chinese medicinal materials are easy to self-assemble to form nanoparticles. The formation of self-assembled nanoparticles(SAN) can not only affect the absorption and distribution of the effective ingredients in Chinese medicinal materials but also may improve the biological activity of the effective ingredients or their simple mixtures, which is of great significance for revealing the compatibility mechanism of Chinese medicine prescription, developing new Chinese medicine products, and producing new nanomaterials. This paper reviews the formation, isolation, characterization, and application of SAN of Chinese medicines, and discusses the problems and development trends of the relevant research, which can provide reference for the further study and promote the innovation and application of such SAN.

Effect of self-assembled nanoparticles from Shaoyao Gancao Decoction on release and absorption of main components of Baishao / 中国中药杂志

To study the effect of self-assembled nanoparticles from Shaoyao Gancao Decoction(SGD-SAN) on the encapsulation, in vitro release and intestinal absorption of the main components of Baishao. Particle size analysis and morphological observation were used to verify the formation of SGD-SAN in the decoction. The entrapment efficiency(EE) of SGD-SAN on the main components of Baishao was determined by ultrafiltration centrifugation. The dialysis bag method was used to study the in vitro release of the main components of Baishao with pH 6.8 phosphate buffer solution as the release media. Single-pass intestinal perfusion study was performed to investigate the effect of SGD-SAN on the absorption of the main components of Baishao. The results showed that there were nanoparticles in the SGD, and the particle sizes and PDI of SGD-SAN were about 200 nm and 0.38, respectively. SGD-SAN was irregularly spherical under transmission electron microscope(TEM). The EEs of albiflorin, paeoniflorin and benzoylpaeoniflorin in SGD-SAN were 33.78%±1.03%,33.61%±0.90%,88.53%±0.58%, respectively. The release characteristics of albiflorin, paeoniflorin and benzoylpaeoniflorin from SGD-SAN showed a slow-release effect on pH 6.8 phosphate buffer solution media. SGD-SAN could significantly enhance the absorption of albiflorin, paeoniflorin and benzoylpaeoniflorin in the ileum. The results of this study indicated that SAN could be formed during the mixed decoction of Baishao and Gancao, and SGD-SAN could encapsulate the components of Baishao, with a certain slow-release effect, and the formation of SAN facilitated the absorption of drugs in the ileum.

Emerging nanoparticulate systems: Preparation techniques and stimuli responsive release characteristics

Nanotechnology has become an outgrowing field in novel drug delivery system. It confers several merits overconventional formulations like increased solubility and bioavailability, targeted drug delivery and a decreaseddose of the drug. The selection of appropriate method for the preparation of nanoparticulate system depends on thephysicochemical characteristics of the drug to be loaded and polymer. This review has covered the most widelyacceptable preparation techniques for polymeric and lipidic nanoparticles including nanoprecipitation, milling,extrusion, supercritical fluid technology, salting out, gelation, sonication, high-pressure homogenization, and solventemulsification methods. Nanocarriers, the traditional nano-formulation drug delivery systems, encountered somemajor problems in process scale-up, reproducibility, and stability during storage. To circumvent these problems a newapproach has emerged which are “In situ or self-assembled nanoparticles drug delivery system.” Such approachescomprise experimentation with different types of polymers, surfactants or novel process in order to prepare a preconcentrate of drug formulation, which on entering into an aqueous medium (gastrointestinal fluid, blood) will formnanoparticles. The in situ nanoformulations can be the futuristic approach in nanocarriers to overcome the problemsassociated with the scale-up process and also minimize the cost of production. This review focuses on differentpreparation techniques for polymeric and lipidic nanocarriers preparation, in situ nanoformulation approaches andrelease characteristics of stimuli responsive nanoformulation

Preparation and characterization of puerarin-loaded polyethyleneimine/sodium alginate nanoparticles / 中草药

Objective To develop the puerarin-loaded polyethyleneimine/alginate nanoparticles (Pur-PEI/ALG-NPs) and investigate their physicochemical properties. Methods The Pur-PEI/ALG-NPs were prepared by electrostatic interaction. The particle size and Zeta potential of nanoparticles were measured by laser light scattering using a Zeta sizer ZEN3600, in vitro release curves for which were studied. The formulation variables were optimized by central composite design-response surface methodology (CCD-RSM) with entrapment efficiency and drug loading as dependent variables. Results An optimal formulation was confirmed as follows: polyethyleneimine concentration was 3.2 mg/mL, alginate concentration was 1.3 mg/mL and the mass ratio of PEI/ALG was 3.75. The resulting nanoparticles exhibited entrapment efficiency of (24.13 ± 1.78)% and drug loading of (11.17 ± 0.71)%, respectively. Zeta potential of nanoparticles was found to be (35.2 ± 0.7) mV, with the average diameter of (118.0 ± 0.4) nm. In vitro release test proved that nanoparticles accelerated the release rate of Pur. Conclusion Pur-PEI/ALG-NPs are prepared successfully with narrow particle size distribution and rich positive charge, which may lay the foundation for further clinical ocular application of Pur.

Preparation and Research on the Aniti-Tumor Activity of Adriamycin Self-assembled Nanoparticles / 浙江中医药大学学报

[Objective] To prepare adriamycin self-assembled nanoparticles, and study the in vivo anti-tumor activity. [Methods]The self-assembled adri-amycin loaded cholesterol-modified pul ulan nanoparticles were prepared by dialysis and were characterized by morphology for particle size,Zeta potential, entrapment efficiency,drug loading content.They were incubated with U251 cel s to assess the inhibition ability of the self-assembled adriamycin-loaded cholesterol-modified pul ulan nanoparticles. [Results]The morphology of self-assembled adriamycin loaded cholesterol-modified pul ulan nanoparticles was spherical. The mean particle size, Zeta potential, entrapment efficiency and drug loading were (112.8 ±1.02)nm,(-27.2±0.246)mV,(67.14±1.21)% and (7.65±0.58)%, respectively.The profiles of release were expressed wel by Higuchi equation. When the dosages were 25μg·mL-1 plus, the inhibiton ability against U251 was stronger than adriamycin solution( P<0.01).[Conclusion]The self-assembled adriamycin loaded cholesterol-modified pul ulan nanoparticles exhibited more cycitoxic activity against U251 than adriamycin solution.