Construction and evaluation of novel self-assembled nanoparticles of Herpetospermum caudigerum Wall / 药学学报

It has become an industry consensus that self-assembled nanoparticles (SAN) are formed by molecular recognition of chemical components in traditional Chinese medicine during the decoction process. The insoluble components in the decoction are mostly in the form of nanoparticles, which can improve the problem of poor water solubility. However, the transfer rate of these insoluble components in the decoction is still very low, which limits the efficacy of the drug. This study aimed to refine the traditional decoction self-assembly phenomenon. The self-assembled nanoparticles were constructed by micro-precipitation method (MP-SAN), and characterized by particle size, zeta potential, stability index and morphology. The formation of MP-SAN and alterations in related physicochemical properties were evaluated using modern spectroscopic and thermal analysis techniques. The quality value transmitting pattern of lignan components within the MP-SAN was assessed via high performance liquid chromatography (HPLC). The MP-SAN showed sphere-like structure with uniform morphology, particle size of (245.3 ± 3.2) nm, polydispersity index (PDI) of (0.13 ± 0.03), zeta potential of (-48.9 ± 5.9) mV and stability index (SI) of (86.05% ± 2.27%). Comprehensive analyses using ultraviolet visible spectroscopy, Fourier transform infrared spectroscopy, differential scanning calorimetry, and other techniques confirmed molecular recognition between the decoction and ethanol extraction, leading to electron rearrangement under the influence of non-covalent bonding. This resulted in the formation of nanoparticles possessing superior thermal stability. As determined by HPLC, the encapsulation rates of the index components in the MP-SAN were all greater than 75% (dehydrodiconiferyl alcohol: 77.00%; herpetolide A: 78.57%; herpetrione: 94.53%), and the transfer rates were all higher than 65% (dehydrodiconiferyl alcohol: 96.01%; herpetolide A: 67.86%; herpetrione: 65.55%), which were 1.34, 1.38 and 4.81 times compared with those of the traditional decoction. In summary, this study successfully constructed the MP-SAN based on micro-precipitation method to achieve high transfer rate and high encapsulation rate of insoluble components in docoction, which provides a pharmaceutics idea for the efficient utilization of pharmacodynamic substance basis of traditional Chinese medicine.

Serum-free cell cryopreservation based on self-assembled peptides / 中国生物制品学杂志

@#Objective To achieve serum-free and low-DMSO efficient cell cryopreservation based on self-assembled peptides(Peptide).Methods Hepa1-6 cells were cryopreserved by combining three cryoprotectants(CPAs),FBS,DMSO and Peptide. Confocal microscopy,flow cytometry and cell counting were used to measure the survival rate,recovery rate and proliferation ability of the cells after freezing,and the ice inhibition of CPAs was tested by differential scanning calorimetry(DSC). Finally,a CPA with high efficiency for cell cryopreservation was determined.Results Peptide formed a fibrous network hydrogel in DMSO solution to encapsulate cells and supported them in a three-dimensional(3D)stereological distribution. Under serum-free conditions,the use of 0. 1 wt% Peptide combined with 5% DMSO as a novel composite CPA for cryopreservation of Hepa1-6 cells significantly improved the survival rate and post-freezing recovery rate compared with the5% DMSO and 0. 1 wt% Peptide groups,and there was no significant difference with the 10% DMSO + 20% FBS group(t =0. 983 and 2. 164,respectively,each P > 0. 05). In addition,compared with the 10% DMSO + 20% FBS group,0. 1 wt%Peptide + 5% DMSO group showed no significant difference in cell proliferation ability after freezing-thawing(t = 3. 513,P > 0. 05). In the end,DSC tests showed that Peptide-based CPA had good ice inhibition performance.Conclusion The use of 0. 1 wt% Peptide combined with 5% DMSO as a novel composite CPA has a good effect on cell cryopreservation.

Advances in applications of molecular dynamics simulation techniques to the research of self-assembled nano-drug delivery systems / 药学学报

Molecular dynamics simulation technology relies on Newtonian mechanics to simulate the motion of molecular system of the real system by computer simulation. It has been used in the research of self-assembly processes illustration and macroscopic performance prediction of self-assembly nano-drug delivery systems (NDDS) in recent years, which contributes to the facilitation and accurate design of preparations. In this review, the definitions, catalogues, and the modules of molecular dynamics simulation techniques are introduced, and the current status of their applications are summarized in the acquisition and analysis of microscale information, such as particle size, morphology, the formation of microdomains, and molecule distribution of the self-assembly NDDS and the prediction of their macroscale performances, including stability, drug loading capacity, drug release kinetics and transmembrane properties. Moreover, the existing applications of the molecular dynamic simulation technology in the formulation prediction of self-assembled NDDS were also summarized. It is expected that the new strategies will promote the prediction of NDDS formulation and lay a theoretical foundation for an appropriate approach in NDDS studies and a reference for the wider application of molecular dynamics simulation technology in pharmaceutics.

Establishment an aggregation-induced emission vesicle material based on supramolecular host-guest chemical assembly for siRNA delivery and study on its toxicity to tumor cells / 国际生物医学工程杂志

Objective:To establish an aggregation-induced emission vesicle material based on supramolecular host-guest chemical assembly (AIE-HG-Vesicle) for siRNA delivery and fluorescence imaging, and to explore its uptake effect by tumor cells and siRNA-based cell killing effect.Methods:By synthesizing β-cyclodextrin modified with polyethyleneimine dendrimer (H-β-CD-dendrimer) as a host compound and a Bola type adamantane containing tetrastyrene AIE group (G-Ada-AIE) as a guest compound, the nanovesicle material was prepared by a supramolecular host-guest self-assembly process for loading siRNA. The morphology and size of the materials were tested by transmission electron microscopy and the dynamic light scattering method. The aggregation-induced luminescence properties of the materials were investigated by fluorescence spectrophotometry. The loading effect of the material on siRNA was investigated by gel retardation experiments. The delivery effect of siRNA-loaded AIE-HG-Vesicle vesicles in tumor cells was observed by a confocal laser scanning microscope. The killing effect of siRNA-loaded AIE-HG-Vesicle vesicles on tumor cells was tested by an MTT assay.Results:The prepared host-guest compounds can be assembled into vesicles with a size of about 100 nm and wall thickness of 9 nm in solution, and the positively charged vesicles on the surface can efficiently load siRNA. The siRNA-loaded AIE-HG-Vesicle vesicles can deliver siRNA into HeLa tumor cells and can be observed through aggregation-induced luminescence. The siRNA-loaded vesicles have an obvious killing effect on HeLa tumor cells.Conclusions:A vesicle material with aggregation-induced luminescence properties was prepared by a method based on supramolecular host-guest chemical assembly, which can be used to deliver siRNA. The material has fluorescence imaging and siRNA-based tumor cytotoxic effects and is expected to be applied to tumor treatment in vivo.

An antigen self-assembled and dendritic cell-targeted nanovaccine for enhanced immunity against cancer

The rise of nanotechnology has opened new horizons for cancer immunotherapy. However, most nanovaccines fabricated with nanomaterials suffer from carrier-related concerns, including low drug loading capacity, unpredictable metabolism, and potential systemic toxicity, which bring obstacles for their clinical translation. Herein, we developed an antigen self-assembled nanovaccine, which was resulted from a simple acryloyl modification of the antigen to induce self-assembly. Furthermore, a dendritic cell targeting head mannose monomer and a mevalonate pathway inhibitor zoledronic acid (Zol) were integrated or absorbed onto the nanoparticles (denoted as MEAO-Z) to intensify the immune response. The synthesized nanovaccine with a diameter of around 70 nm showed successful lymph node transportation, high dendritic cell internalization, promoted costimulatory molecule expression, and preferable antigen cross-presentation. In virtue of the above superiorities, MEAO-Z induced remarkably higher titers of serum antibody, stronger cytotoxic T lymphocyte immune responses and IFN-γ secretion than free antigen and adjuvants. In vivo, MEAO-Z significantly suppressed EG7-OVA tumor growth and prolonged the survival time of tumor-bearing mice. These results indicated the translation promise of our self-assembled nanovaccine for immune potentiation and cancer immunotherapy.

Electrochemical immunosensing of low-density lipoprotein based on sol-gel encapsulation

Abstract Lipoprotein monitoring is desirable in the management of medical conditions such as atherosclerotic cardiovascular disease and coronary artery disease, in which controlling the concentration of these chylomicrons is crucial. Current clinical methods are complex and present poor reproducibility between laboratories. For these reasons, recent guidelines discard the assessment of low-density lipoprotein cholesterol (LDL-C) as a routine analysis during lipid-lowering therapies. Concerning the importance of monitoring this parameter, the authors present an electrochemical immunosensor constructed from a simple and easy-to-reproduce platform that allows detecting and quantifying LDL nanoparticles directly from human serum samples. The performance of the biosensor was studied by scanning electron microscopy, cyclic voltammetry, and electrochemical impedance spectroscopy. The biosensing platform displays good stability and linearity between 30 mg dL-1 and 135 mg dL-1 with a detection limit of 20 mg dL-1. The proposed biosensor can be easily employed for monitoring LDL concentration in clinical treatments.

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.

An Overview On Aquasomes : A Novel Approach For Delivering Macromolecules

In recent blossoming era of research in nanobiotechnology, aquasomes are viewed as an effective and efficient carrier system for drug delivery or biochemically active long chain macromolecules like protein and peptide, different hormones, antigens, enzymes and gene delivery. Aquatones are spherical in shape and having particle size within 60- 300nm. Self-assembled structure of aquasome (due to its natural property) it generates a focus on nanobiotechnology research as a carrier system. Mainly, aquasomes contain three-layers, that is core material, coating material, drug layer attached by ionic or non-covalent bond. Aquasomes include mainly the core materials like , hydroxyapatite, solid phase nanocrystalline ceramic diamond (carbon) and calcium phosphate dihydrate(brushite) . The coating of core material is done with glassy polyhydroxyl oligomeric film such as cellobiose and trehalose, on which modification of biochemically active molecules are attached. Whereas, calcium phosphate used as a core material, because of it is naturally present in the body.Whether calcium phosphate is unstable in nature, due to prolong storage it converts into hydroxyapatite which is a better core than calcium phosphate to develop the aquasomes. The solid core material renders stability of structures, while the coating material stabilizes the biochemically active molecules and protects against dehydration. In this review, we tried to an overview of aquasomes, and about its advantages over conventional drug delivery system, shielding effect of aquasomes on desired drug and how its self-assembled structures, makes them an attractive carrier to deliver biochemically active molecules.

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 .

Application of supramolecular peptide self-assembly in biomedicine / 生物工程学报

In recent years, peptide self-assembly has received much attention because of its ability to form regular and ordered structures with diverse functions. Self-assembled peptides can form aggregates with defined structures under specific conditions. They show different characteristics and advantages (e.g., good biocompatibility and high stability) compared with monomeric peptides, which form the basis for potential application in the fields of drug delivery, tissue engineering, and antiseptics. In this paper, the molecular mechanisms, types and influencing factors of forming self-assembled peptides were reviewed, followed by introducing the latest advances on fibrous peptide hydrogels and self-assembled antimicrobial peptides. Furthermore, the challenges and perspectives for peptide self-assembly technology were discussed.

Self-assembled aggregations in Coptidis Rhizoma decoction dynamically regulate intestinal tissue permeability through Peyer's patch-associated immunity / 中草药·英文版

Objective: To investigate the dynamic regulation of self-assembled aggregations (SAA) in Coptidis Rhizoma decoction on the permeability of intestinal tissue and the mechanism underlying. Methods: The effects of SAA on berberine (Ber) absorption were respectively analyzed in an in situ intestinal perfusion model and in an Ussing Chamber jejunum model with or without Peyer's patches (PPs). The expression levels of ZO-1, Occludin and Claudin-1 were detected by immunofluorescence to evaluate the tight junction (TJ) between intestinal epithelium cells. The expression levels of T-box-containing protein expressed in T cells, signal transducers and activators of tranion-6, retinoic acid receptor-related orphan receptor γt and forkhead box P3 in PPs were detected by the reverse transcription-polymerase chain reaction and the secretions of interferon-γ (IFN-γ), interleukin-4 (IL-4), interleukin-17 (IL-17) and transforming growth factor-β (TGF-β) in PPs were evaluated by immunohistochemistry, to reflect the differentiation of T lymphocyte in PPs to helper T (Th) cell 1, Th2, Th17 and regulatory T (Treg) cell. To confirm the correlation between SAA in Coptidis Rhizoma decoction, PPs-associated immunity and intestinal epithelium permeability, SAA were administrated on an Ussing Chamber jejunum model with immunosuppressed PPs and evaluated its influences on intestinal tissue permeability and TJ proteins expression. Results: SAA in Coptidis Rhizoma decoction could dose-dependently promote Ber absorption in jejunum segment, with the participation of PPs. The dose-dependent and dynamical regulations of SAA on permeability of intestinal tissue and TJ proteins expression level between intestinal epithelium cells occurred along with the dynamically changed T lymphocyte differentiation and immune effectors secretion in PPs. The administration of SAA on immunosuppressed PPs exhibited dose-dependent PPs activation, inducing dynamic promotion on intestinal tissue permeability and inhibition on TJ proteins expression. Conclusion: SAA can improve the Ber absorption in small intestine, through the PPs-associated immunity induced dynamic regulation on intestinal tissue permeability and TJ proteins expression. These findings might enlighten the research of traditional Chinese medicine decoction.

Research progress in nanomaterials in hemostasis / 药学实践杂志

Nanomaterials, with the advantages of unique microstructure, have been widely used in the fields of material manufacturing, microelectronics and computer technology, medicine and health, environment and energy. Compared with traditional hemostatic materials, nanomaterials can improve the bioavailability and stability of traditional hemostatic drugs to a certain extent, enhance the controlled and targeted release of drugs, which lay a good foundation for the development of new-style modern hemostatic nanomaterials. This paper reviews the advanced design and application progress of various nanomaterials in hemostasis, such as liposomes, nanoparticles, self-assembled nano peptides, nanofibers, etc. Finally, the challenges and prospects of hemostatic nanomaterials are briefly described.

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.

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.

Study on the Effects of Self-assembly Micelles of Euphorbiae Semen Fatty Oil on Intestinal Absorption of 4 Kinds of Euphorbia in Rats / 中国药房

OBJECTIVE：To study the effects of different amounts of Euphorbiae Semen fatty oil in self-assembly micelles on intestinal absorption of 4 kinds of euphorbia （euphorbia L 1，L2，L3，L8）in rats. METHODS ：The self-assembled micelle solution containing 4 kinds of euphorbia was prepared by adding 4 kinds of euphorbia （40 mg/L）in excess ，using the fatty oil of Euphorbia Semen（0.2，0.4，1，4 g/L）and sodium deoxycholate as carriers. Totally 60 rats were collected to establish in-situ one-way intestinal perfusion model. Different intestinal segments （duodenum，jejunum，ileum，colon）were perfused with drug-containing intestinal perfusion fluid according to different dosage of Euphorbiae Semen fatty oil. HPLC method was adopted to determine the contents of 4 kinds of euphorbia in the intestinal perfusate before and after perfusion. The absorption rate constant （Ka）and apparent absorption coefficient （Peff）of 4 kinds of euphorbia in different intestinal segments were calculated. The ileum segment with better absorption was selected as the object to investigate and calculate the ac cumulative absorption of 4 kinds of euphorbia. RESULTS：The self-assembled micelles formed by different concentrations of fatty oil of Euphorbiae Semen could significantly increase the absorption of 4 kinds of euphorbia in different intestinal segments to different extents. When the dosage of Euphorbiae Semen fatty oil was 0.4 g/L，the intestinal absorption effect of 4 kinds of euphorbia were all the best ；the Peff was significantly increased，compared with no fat oil group （P＜0.05 or P＜ . According to the order of Ka and Peff of each intestinal ： segment in different fatty oil dosage groups ，the absorption 0531-89628590。E-mail：1310394709@qq.com effect of 4 kinds of euphorbia in each intestinal segment was the best in jejunum and the worst in colon. Compared with no fatty oil group ，when the amount of Euphorbiae Semen fatty oil w as 0.2-4 g/L，accumulative amount of 4 kinds of euphorbia in the ileum of rats increased significantly （P＜0.05 or P＜0.01）， and the highest in 0.4 g/L Euphorbiae Semen fatty oil group. CONCLUSIONS ：The self-assembly micelle s composed of Euphorbiae Semen fatty oil and deoxycholate can increase the absorption of euphorbia L 1，L2，L3，L8 in each intestinal segment to different extent，and the jejunum is the main absorption segment.

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

Effect of processing excipient suet oil on formation and absorption of baohuoside Ⅰ-bile salt self-assembled micelles / 中国中药杂志

The fried method with suet oil,which can strengthen the effect of Epimedium in warming kidney and enhancing Yang,has been widely used in the processing of Epimedium in traditional Chinese medicine. Based on the formation mechanism of Epimedium flavonoids self-assembled micelles in vivo,the synergistic mechanism of processing excipient suet oil was investigated in this paper from the perspective of pharmaceutics. Baohuoside Ⅰ,as representative component of processed Epimedium,was selected as model drug.Average size and zeta potential were measured and the morphology of micelles was observed under transmission electron microscopy. Caco-2 monolayer cell model,rat intestinal perfusion model and in vivo serum drug concentration method were established to investigate the effect of suet oil on the formation and absorption of the baohuosideⅠ bile salt self-assembled micelles. Baohuoside Ⅰ can form selfassembled micelles under the action of sodium deoxycholate. While,adding suet oil into the baohuoside Ⅰ-bile salt micelles( BSDOC) can make it form a more stable system with a smaller average size,higher Zeta potential,lower polydispersity index( PDI) value,significantly improved encapsulation efficiency and drug loading,indicating that suet oil could significantly improve the micelle formation in vivo. In addition,the permeability coefficient of baohuoside Ⅰ in Caco-2 monolayer cells and the four intestinal organs( duodenum,jejunum,ileum and colon) was increased and the oral bioavailability was also improved after adding the suet oil to BS-DOC.All the results demonstrated that the suet oil can promote the formation and absorption of baohuoside Ⅰ self-assembled micelles,so as to enhance its synergistic effects.

Effects of staurosporine on the contraction of self-assembled constructs of goat temporomandibular joint disc cells / 华西口腔医学杂志

OBJECTIVE@#The effects of the staurosporine on contraction of self-assembled constructs and extracellular matrix syntheses of goat temporomandibular joint discs were investigated.@*METHODS@#Goat temporomandibular joint disc cells were isolated and cultured to P3, and 5.5×10⁶ cells were combined with different concentrations of staurosporine (0, 0.1, 1, 10, 100 nmol·L⁻¹) in agarose wells and cultured for one week. The samples were frozen and sectioned. Safranin-O,  Picro-sirius red and immunohistochemical staining were performed to observe the distributions of the extracellular matrix and the expression of alpha-smooth muscle actin (α-SMA). Enzyme linked immunosorbent assay (ELISA) and Blyscan kits were utilized to quan--titatively detect the contents of type Ⅰ collagen (ColⅠ) and glycosaminoglycans (GAGs).@*RESULTS@#Each group of goat temporo-mandibular joint disc cells in the agarose wells were gathered to self-assemble into a disc-shaped base for 4 hours and then to gradually contract into a round shape. The Picro-sirius red staining was strong and indicated collagen distribution. The Safranin-O staining observed GAGs throughout the entire construct. The expression of ColⅠ was strongly posi-tive in the staurosporine groups; however, the expression of α-SMA was weak. ColⅠ and GAGs contents in the stau-rosporine groups were greater than that of the control group, especially in the 10 nmol·L⁻¹ group (P<0.01).@*CONCLUSIONS@#Staurosporine has a certain effect on the shrinkage of self-assembled constructs; however, such effect is not prominent. Staurosporine contributes to the construction synthesis of extracellular matrix.

Structure of the Conjugated Linoleic Acid-Paclitaxel Conjugate Self-Assembled Nanoparticles / 中国药学杂志

OBJECTIVE: To prepare, the conjugated linoleic acid-paclitaxel conjugate self-assembled nanoparticles (CLA-PTX NPs) by nanoprecipitation. METHODS: The Dynamic light scattering, nuclear magnetic resonance spectroscopy, raman spectroscopy, fourier transform infrared spectroscopy and nitrogen element distribution of CLA-PTX NPs were studied. RESULTS: The hydroxyl groups (C-4 and C-10 of PTX) and the acetyl groups (C-1 and C-7 of PTX) were on the surface of CLA-PTX NPs, CLA carbon chain, the benzene ring (C-2 and C-3' of PTX) and the amide bond (C-3' of PTX) were inside the CLA-PTX NPs. CONCLUSION: It is speculated that the self-assembly of CLA-PTX is that the non-polar CLA carbon chain spontaneously aggregates inward due to hydrophobic interaction, and the hydrophilic oxygen-containing groups of PTX (hydroxyl group and carbonyl group) are on the surface of the nanoparticle to form nanoparticles.

A novel tissue engineering complex——BMSCs Sheet-RADA16 scaffold constructed by cell sheet and self-assembled peptides technique / 实用口腔医学杂志

Objective: To construct a novel tissue engineering complex, BMSCs sheet-RADA16 scaffold, by combining cell sheet and self-assembled peptides.. Methods: The self-assembled peptide RADA16 scaffold was wrapped with the BMSCs cell sheet. The morphology of the cells and the complex were observed by SEM and confocal laser microscopy, and the proliferation of cells was assessed by CCK-8. The osteogenic differentiation of BMSCs was examined by detection of related gene expression with RT-PCR. Results: Compared with the BMSCs cell sheet, the numbers of cells on RADA16 scaffold growth rapidly at 3 rd-8 th day, and BMSCs were more on the scaffold than those on the cell sheet (P＜0. 05) . RT-PCR results showed that the expression level of osteogenesis-related genes was higher in the complex (P＜0. 05) . Conclusion: BMSCs Sheet-RADA16 Scaffold may promote proliferation and osteogenic differentiation of BMSCs.