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In view of the longevity and innate immune escape of red blood cells, this study designed the red blood cell membrane-coated paclitaxel nanosuspension [RBC-(PTX)NS] and investigated its physicochemical properties and antitumor effect in vitro. Paclitaxel nanosuspension [(PTX)NS] was prepared by ultrasonic precipitation and then RBC-(PTX)NS by ultrasonic coating. The formulation of(PTX)NS was optimized with Box-Behnken method and indexes of particle diameter, zeta potential, and stability. The morphology, particle diameter, stability, in vitro dissolution, and antitumor effect of(PTX)NS and RBC-(PTX)NS were characterized. The results showed that the particle diameter and zeta potential were(129.38±0.92) nm and(-22.41±0.48) mV, respectively, for the optimized(PTX)NS, while(142.5±0.68) nm and(-29.85±0.53) mV, respectively, for RBC-(PTX)NS. Under the transmission electron microscope,(PTX)NS was spherical and RBC-(PTX)NS had obvious core-shell structure. RBC-(PTX)NS remained stable for 5 days at 4 ℃. The in vitro dissolution test demonstrated that the cumulative release rate of RBC-(PTX)NS reached 79% within 20 min, which was significantly higher than that(25%) of(PTX)NS(P<0.05). As evidenced by MTT assay, RBC-(PTX)NS highly inhibited the proliferation of HepG2 cells in a dose-dependent manner. The cell membrane-coated nano-preparation preparation method is simple and reproducible. It improves the solubility of PTX and endows RBC-(PTX)NS with higher stability and stronger cytotoxicity. Thus, it is a new method for the delivery of PTX via nanocrystallization.
Subject(s)
Erythrocyte Membrane , Nanoparticles/chemistry , Paclitaxel/pharmacology , Particle Size , SuspensionsABSTRACT
Objective To prepare isophenylcyclopentylamine hydrochloride capsules and evaluate its quality. Methods The suitable excipients were selected by the drug-excipient compatibility test,and after the formulation and preparation process design and screening,the micromeritic property and hygroscopicity of contents of capsules as well as the basic performance and stability of is-ophenylcyclopentylamine hydrochloride capsules were evaluate. Results The selected formulation was composed of isophenylcyclo-pentylamine hydrochloride 10 mg,anhydrous dibasic calcium phosphate 128.7 mg,mannitol 128.7 mg and aerosil 2.7 mg.The angle of repose of intermediate powders was(30.71±1.09)°,aerated and packed bulk densities were(0.76±0.01)and(0.90±0.02)g/ml re-spectively,Hausner value was 1.19±0.01,Carr′s index was(15.86±1.05)%,indicating good flowability and filling property as well as relatively low humidity.The contents,uniformity of contents and dissolution of capsules fulfilled the requirements.The quality of ca-pusles kept well in the 6-month accelerated and long-term stability test.Conclusion The formulation is simple and reasonable,and the preparation process showed a good reproducibility,which might be suitable for industrialization.
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Objective To perform a preformulation study for a new antirheumatic drug DK-507 so as to provide theoretical basis for its preparation research.Methods The appearance,crystal form and solubility of DK-507 were investigated.A high perfor-mance liquid chromatography(HPLC)method for the quantitative determination of DK-507 was established.The apparent oil/water (O/W)partition coefficient of DK-507 and the equilibrium solubility of the drug under different pH conditions were determined. Re-sults DK-507 is a white crystalline powder,which is odorless,tasteless and insoluble in water.The quantitative HPLC method for the DK-507 determination showed a good linearity in the range of 10-80 μg/ml(R=0.9998).The apparent O/W partition coefficient of DK-507 was determined to be 1.80.In the different pH solutions,the solubility of DK-507 showed a W-form change,with poor solubili-ties in lower pH solutions,which showed a gradient improvement with the increase of the solution pH values.Conclusion The quanti-tative HPLC method for the DK-507 determination,established in this study,is accurate and reliable.The present results indicate that DK-507 is a water-insoluble drug,and according to the O/W partition coefficient,DK-507 seems likely to be prepared into oral solid preparations.
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Objective To optimize the conditions for the synthetic process of iron sucrose complex (ISC), via the investigation of the effects of reaction temperature (X1), reaction time (X2), amount of alkali (X3), and amount of sucrose (X4) on the relative molecular mass of the ISC product. Methods According to the experimental results for the single factor, the conditions dealing with the X1, X2, X3, and X4 parameters for the preparation of ISC were optimized by the Box-Behnker design combined with the response surface methodology using the weight average relative molecular mass of ISC as an indicator, and analyzed with gel permeation chromatography. Results The reaction temperature and the amount of alkali had a significant effect on the weight average relative molecular mass of ISC. The influence of the four factors in the descending order was as follows:X3＞X1＞X2＞X4. In the designed experimental conditions, theresponsevaluedecreasedwiththeincreaseofbothreactiontemperaturesandalkaliamounts. Conclusion Theresponse surface methodology could provide the relationship between the response values and variables via the minimum number experiments to obtain the optimized conditions for the preparation of ISCs.
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Objective To establish an HPLC method for the determination of anti-influenza drug GZ830 and its related substances, and investigate the degradation of GZ830. Methods The degradation of GZ830 under the conditions with different pH and temperatures was investigated with HPLC method to explore the degradation principle. Results The HPLC method for the determination of GZ830 was established. The linear relationship between the drug and the peak area was good in the concentration range of 160-1200 μg/ml (r=0.9998). GZ830 was easily degraded under alkaline conditions and could not tolerate high temperatures. The degradation of GZ80 did not occur when its aqueous solution was kept at 40℃ for 6 h. However, after heating at 80℃ for 6 h, about 2.4％GZ80 was degraded and the degradation rate reached about 7％ after kept at 115℃ for 30 min. Conclusion Under the optimized chromatographic conditions, GZ830 was well separated from the degraded products, and the HPLC method possessed high sensitivity and good specificity for the determination of GZ80, and the degradation of GZ80 was different under different conditions.
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To deal with effectively acute chemical injury events, the service ability of protective medicine against chemical weapons has being widened from dealing with traditional chemical warfare to public chemical accident or chemical terrorist attack. Focusing on the important researching and developing of medicine for chemical defense use only, the novel drug/device combination products should be vigorously promoted including the new mechanism, good curative effect and high safety of detoxification drugs such as hydroxycobalamin used in the treatment of known or suspected cyanide poisoning in both adults and the pediatric population, and the convenient and quick drug delivering technologies such as auto-injectors with a retreat hidden needle and a smart remindful injection, which could improve greatly the emergency medical rescue ability of chemical accidents.
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Oral modified-release multiple-unit dosage forms such as coated pellets have always been more effective therapeutic alternative to conventional single-unit dosage forms. Coated pellets ranging in size, typically, between 0.5-1.0 mm, are produced primarily for the purpose of oral controlled-release dosage forms having gastro-resistant or sustained-release properties or the capability of site-specific drug delivery. With regards to the final dosage form, the multi-particulates are usually formulated into single-unit dosage forms such as filling them into hard gelatin capsules or compressing them into tablets. As drug-delivery systems become more sophisticated, the role of pellets in the design and development of dosage forms is increasing. The safety and efficacy of the formulation is higher than that of other dosage forms. This review provides an update on this research area and discusses the phenomena and mechanisms of the multi-particulate system concluding multiple-unit pellet system and pellet-containing tablets.
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Auto-injector, a spring-driven drug-device based combination production that automatically injects the drug into the skin via a pre-filled syringe or cartridge, allows minimally trained individuals to self-inject potentially life-saving medication when emergency medical care may be absent or remote, and thus has been becoming a supporting approach of emergency medicine for the first-aid. The auto-injector was developed originally by the United State of America, and experienced the three outstanding states including syrettes, single chamber auto-injectors and dual chamber auto-injectors from the battlefield to the civilianization. The current auto-injector devices have five different types named as ACE (AtroPen), ComboPen, Binaject, Soluject and Truject, respectively. The applied drugs to the systems for military use have atropine, pralidoxime chloride, obidoxime, diazepam and morphine sulfate. The other drugs for emergency medical use such as epinephrine, lidocaine hydrochloride and sumatriptan have been also applied to. All of the auto-injector based combination production have been twined with a simulator in order to conduct a training schedule before use. Importantly, the needle hidden or the device-status notification technique after injection has been becoming a trend in the technology advances of the auto-injectors.