Preparation of vitexin albumin nanoparticles and its pharmacokinetic study / 中国中药杂志

This study aims to prepare vitexin albumin nanoparticles(VT-BSA-NPs) to alleviate the low bioavailability of vitexin(VT) in vivo due to its poor water solubility. VT micro powders were prepared by the antisolvent crystallization method, and the morphology, size, and physicochemical properties of VT micro powders were studied. The results showed that the VT micro powder had a particle size of(187.13±7.15) nm, an approximate spherical morphology, and a uniform size distribution. Compared with VT, the chemical structure of VT micro powders has not changed. VT-BSA-NPs were prepared from VT micro powders by desolvation-crosslinking curing method. The preparation process was screened by single factor test and orthogonal test, and the quality evaluation of the optimal prescription particle size, PDI, Zeta potential, EE, and morphology was performed. The results showed that the average particle size of VT-BSA-NPs was(124.33±0.47) nm; the PDI was 0.184±0.012; the Zeta potential was(-48.83±2.20) mV, and the encapsulation rate was 83.43%±0.39%, all of which met the formulation-related requirements. The morphological results showed that the VT-BSA-NPs were approximately spherical in appearance, regular in shape, and without adhesion on the surface. In vitro release results showed a significantly reduced release rate of VT-BSA-NPs compared with VT, indicating a good sustained release effect. LC-MS/MS was used to establish an analytical method for in vivo analysis of VT and study the plasma pharmacokinetics of VT-BSA-NPs in rats. The results showed that the specificity of the analytical method was good, and the extraction recovery was more than 90%. Compared with VT and VT micro powders, VT-BSA-NPs could significantly increase AUC, MRT, and t_(1/2), which was beneficial to improve the bioavailability of VT.

Design, Development And Characterization Of Curcumin Loaded Albumin Nanoparticles For The Treatment Of Parkinson’s Disease

Curcumin being component of Curcuma longa is a natural polyphenol. Observing on a chemical level, curcumin is a natural polyphenol which is denominated (1E,6E)-1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene3,5-dione) which is usually extracted through the rhizomes of Curcuma longa. Structurally, it is composed of a trio of chemical identities on a molecular level: dual aromatic ring system. The objective of the research was to design, development and characterization of herbal drug loaded albumin nanoparticles to cure parkinson’s disease for improving and increasing the therapeutic efficacy and also reducing the frequency of dose. The optimized formulations were obtained after applying the design of experiment which was Box Behnken method where three independent variables; polymer concentration, stirring time, crosslinker concentration were selected. Curcumin nanoparticles loaded with albumin were formulated by ph coacervation method in which ethanol was used as desolvating agent along with a cross linking agent (Glutaraldehyde) and albumin as the polymer. The particle size and polydispersity index of curcumin loaded albumin nanoparticles was measured via dynamic light scattering technique. Drug release research conducted using in vitro method over the duration of 24 hours. Ex vivo drug release study of the albumin nanoparticles was performed using nasal membrane of goat. It has been shown that in case of hydrophilic matrices, swelling of polymer occurs followed by release of drug by diffusion which was best explained by Korsmeyer- peppas equation, which indicates drug release through diffusion which occurs by swelling of polymer matrix and remained constant throughout the release of drug in body. By virtue of particle size, the designed nanoparticles effortlessly goes into the nasal mucosa.

Biopolymer Nanoparticles: A Review of Prospects for Application as Carrier for Therapeutics and Diagnostics

Biopolymer nanoparticles are molecules of interest in the direction of generation of new pre-diagnostic and treatmentstrategies with improved efficacy and specificity. Several methods have been developed to produce biopolymernanoparticles. These biopolymer nanoparticles had distinct properties such as size and charge according to the productionmethod affecting their targeting and drug encapsulation abilities. The present review highlighted the progress in thedevelopment of theronostic nanoparticles. The surface of the nanoparticles may be subjected to modification and be hiddenfrom the immune system, so that they can stay in blood circulation for a long time to achieve their intended outcome. Thesafety and efficacy of most of the generated nanoparticles systems were not tested in humans in details. The synthesizablenanoparticles that are generated using biodegradable and/or biocompatible building blocks have been easy to be consideredas important candidates for the usage in treatment and diagnostic evaluation plan. In-depth understanding and researchmust be achieved for better understanding of the mechanism of theranostic nanoparticles metabolism and their excretion outof the human body. An attempt to summarize the recent research studies in the field of therapeutics and diagnostics based onthe biopolymers was achieved in this review article

Optimization of Formulation of Co-loaded Docetaxel and Gambogic Acid Albumin Nanoparticles and Evaluation of Its Quality / 中国实验方剂学杂志

Objective: The formulation of co-loaded docetaxel(DTX) and gambogic acid(GA) albumin nanoparticles(DTX-GA-BSA NPs) was optimized by central composite design-response surface methodology to prepare DTX-GA-BSA NPs, and its quality was evaluated. The optimal synergistic ratio of DTX and GA was screened by coefficient of drug interaction(CDI). Method: NabTM method was used to prepare DTX-GA-BSA NPs with bovine serum albumin(BSA) as the carrier material. Design-Expert 8.0.6 software was used to design the experiment and process the data, overall desirability(OD) of particle size and polydispersity index(PDI), encapsulation rate were taken as indexes. The particle size and Zeta potential of the nanoparticles were measured. Individual and synergistic inhibitory effects of DTX and GA on the proliferation of MGC-803 and HGC-27 cells were determined by methyl thiazolyl tetrazolium(MTT) assay, respectively. Result: The optimum prescription of DTX-GA-BSA NPs was as follows:BSA concentration of 5 g·L-1, water-oil phase volume ratio of 1:17, drug-loading ratio(mass ration of drug to carrier) of 1:10.The average particle size of DTX-GA-BSA NPs was 135.8 nm and PDI was 0.09, Zeta potential was -21.4 mV. The deviation between the predicted value and the observed value of the model was small, the model had good predictability. For MGC-803 cell, when the concentrations of DTX and GA were 0.004, 0.12 μmol·L-1, respectively(mass ratio of DTX to GA was 1:23), the CDI value was the smallest and the synergistic proliferation inhibition was the most significant. For HGC-27 cell, when the concentrations of DTX and GA were 0.004, 1 μmol·L-1, respectively(mass ratio of DTX to GA was 1:195), the synergistic proliferation inhibition was the most significant. Conclusion: The optimized formulation of DTX-GA-BSA NPs is stable and reliable. The established mathematical model has good predictive ability and practicability. DTX combined with GA has synergistic effect on MGC-803 and HGC-27 cells without concentration dependence.

Preparation, characterization, and antiproliferative activities of biotin-decorated docetaxel-loaded bovine serum albumin nanoparticles

ABSTRACT The aim of the present study was to characterize biotin-decorated docetaxel-loaded bovine serum albumin nanoparticles (DTX-BIO-BSA-NPs) and evaluate their antiproliferative activity in vitro. The particle size of prepared DTX-BIO-BSA-NPs was found to be always lower than 200 nm, with sizes of 166.9, 160.3, 159.0, 176.1 and 184.8 nm and the zeta potential was -29.51, -28.54, -36.54, -36.08 and -27.56 mV after redissolution with water for 0, 1, 2, 4 and 8 hours, respectively. The polydispersity index (PDI) was stable in the range of 0.170 - 0.178. In the in vitro drug-release study, the DTX-BIO-BSA-NPs targeted a human breast cancer cell line MCF-7 effectively. The x-ray diffraction spectrum and DSC curve of DTX-BIO-BSA-NPs suggested that docetaxel was in an amorphous or disordered crystalline phase in DTX-BIO-BSA-NPs. In vitro cytotoxicity results showed that DTX-BIO-BSA-NPs inhibits proliferation of MCF-7, SGC7901, LS-174T and A549 cells in a concentration-dependent manner after exposure to DTX-BIO-BSA-NPs for 48 hours. Taken together, these results indicate that DTX-BIO-BSA-NPs may have potential as an alternative delivery system for parenteral administration of docetaxel.

Preparation and Quality Evaluation of Norcantharidin Albumin Nanoparticles / 中国药师

Objective: To prepare norcantharidin albumin nanoparticles and evaluate the physical characteristics of the albumin nanoparticles. Methods:Norcantharidin albumin nanoparticles were prepared by ultra-high pressure microfluidization technology. The average particle size and the drug entrapment efficiency of albumin nanoparticles were used as the evaluation indices. Firstly,Plackett-Burman experimental design was used to screen the formula and process variables which had significant effects on the properties of albu-min nanoparticles,and then Box-Behnken experimental design was used to optimize the variables range. The morphology,particle size distribution,zeta potential and in vitro drug release behavior were investigated. Results:The average particle size of norcantharidin al-bumin nanoparticles was (105.2 ± 30.1) nm,the PdI was 0.127,and the zeta potential was( -24.7 ± 1.9) mV. In 0.5% Tween-80 phosphate buffered saline (pH 7.4),the in vitro cumulative release of norcantharidin albumin nanoparticle suspension reached up to 81.4% in 24 h. Conclusion:The preparation technology of norcantharidin albumin nanoparticles by ultra-high pressure microfluidi-zation technology is simple and feasible. The preparation technology can be used in industrial production.

Preparation and antitumor effects of tanshinone ⅡA loaded albumin nanoparticles / 中国中药杂志

In this study, the tanshinone ⅡA loaded albumin nanoparticles were prepared by high pressure homogenization method. The formulation was optimized by central composite design-response surface method (CCD-RSM), with the particle size, encapsulation efficiency, and drug loading as indexes to investigate their in vitro anti-tumor effect. The results showed that the prepared nanoparticles had uniformly spherical morphology and uniform particle size distribution. The average particle size, encapsulation efficiency and drug loading of nanoparticles were about (175.7± 3.07) nm, 90.8%±1.47% and 5.52%±0.09%, respectively. Tanshinone ⅡA loaded albumin nanoparticles showed a more powerful antitumor effect than free tanshinone ⅡA for human promyelocytic leukemia NB4 cells. The preparation method of the drug-loaded albumin nanoparticles was simple and easy, and can significantly improve the solubility of tanshinone ⅡA, so it was helpful to extend its application in therapies against hematological malignancies.

Pharmacokinetics and Tissue Distribution of Voriconazole Albumin Nanoparticles in Rats / 中国药师

Objective: To prepare voriconazole albumin nanoparticles and evaluate the characteristics of pharmacokinetics and tissue distribution in rats.Methods: Voriconazole albumin nanoparticles were prepared by a new ultra-high pressure microfluidization technology.The physicochemical properties of voriconazole albumin nanoparticles were studied, such as the particle size distribution, zeta potential and particle shape.The release of voriconazole from albumin nanoparticles was investigated in pH7.4 phosphate buffered saline.The concentrations of voriconazole in plasma and the other different tissues were determined after the tail-vein injection of voriconazole albumin nanoparticles in rats.Results: Voriconazole albumin nanoparticles were homogeneous small spheres as seen under a transmission electron microscope.The average particle diameter was (121.9±41.6) nm, the polydispersity index was 0.197, and the zeta potential was (-42.1±0.9) mV.In 0.5% Tween-80 phosphate buffered saline (pH7.4), the in vitro cumulative release of voriconazole albumin nanoparticles reached up to 67.5% in 24 h.AUC0-24 of voriconazole albumin nanoparticles and voriconazole injection was (98.27±1.42) and (105.32±1.45) g/L/h, and MRT0-24 was (4.48±0.38) and (4.86±0.51) h, respectively.Conclusion: Voriconazole albumin nanoparticles can prolong the circulation time, and exhibit promising targeting ability in liver, spleen and brain.

Preparation and in vitro evaluation of albumin nanoparticles produced by thermal driven self-assembly / 中国药科大学学报

@#The aim of this study was to prepare albumin nanoparticles by thermal driven self-assembly, and to investigate the formation mechanism, cellular uptake, the kinetics of cellular uptake and intracellular degradation, etc. By measuring the concentrations of thiol, amino and carboxyl groups, the formation mechanism of albumin nanoparticles was revealed. CCK-8 assay was performed to detect the cytotoxicity; inverted fluorescence microscope was used to observe the cellular uptake of the nanoparticles; while the fluorescence resonance energy transfer(FRET)method was applied to investigate the cellular uptake and intracellular degradation kinetics. The drug-loading capacity was investigated using paclitaxel(PTX)as the model drug. The results showed that the albumin nanoparticles produced by thermal driven self-assembly were safe, nontoxic, biodegradable and stabilized by intermolecular disulfide and amide bonds. The drug-loading study indicates that PTX can be highly encapsulated in the nanoparticles. Hence, thermal driven self-assembly method is green and easy to operate, and the albumin nanoparticles can be applied as a new delivery platform for anticancer drugs.

Design, development and characterization of serratiopeptidase loaded albumin nanoparticles.

In recent years, albumin nanoparticles have been widely studied for delivery of various active pharmaceuticals with enhanced accumulation at the site of inflammation. Albumin is a versatile carrier to prepare nanoparticles and nanospheres due to its easy availability in pure form, biodegradability non-toxic and non-immunogenic nature. The mechanism of action of Serratiopeptidase appears to be hydrolysis of histamine, bradykinin and serotonin. Serratiopeptidase also has a proteolytic and fibrinolytic effect. Protein i.e. bovine serum albumin was used to entrap serratiopeptidase enzyme. Protease activity of the enzyme was checked and method was validated to access the active enzyme concentration during formulation. Solvent desolvation method was used for the preparation of BSA nanoparticles. Effect of buffer pH was checked on the enzyme activity. Chloroform was selected and used as solvent for nanoparticle preparation. Effect of various variables such as concentration of BSA, agitation rate, glutarldehyde concentration, time of crosslinking etc. on the formulation was studied. Formed nanoparticles were characterized for drug content, in-vitro release, entrapment efficiency, particle size and size distribution. The formed serratiopeptidase loaded albumin nanoparticles may be used for the treatment of arthritis.