Development of an oral rutin nanocrystal formulation

Dried rutin nanocrystals have been prepared by lyophilization and investigated regarding their physicochemical properties with respect to re-dispersability, particle size, morphology and dissolution behavior. Photon correlation spectroscopy (PCS) and laser diffractometry (LD) were employed to determine the particle size. Morphology of the particles was analyzed by light microscopy. Lyophilized rutin nanocrystals were incorporated into tablets and the dissolution behavior of the tablets was evaluated. Very fine particles of lyophilized rutin could be completely re-dispersed in the water. The PCS size average and polydispersity index (PI) of lyophilized rutin were of 721 nm and of 0.288 after re-dispersion. The rutin nanocrystal-loaded tablets were produced using direct compression. The dissolution velocity of the rutin nanocrystal-loaded tablet was superior compared to rutin microcrystal-loaded and a marketed tablet. After 30 min rutin was released and dissolved completely from the nanocrystal tablets in water. In contrast, only 71% and 55% of the total amount of rutin were dissolved from the microcrystal tablets and the marketed tablet, respectively. The improving dissolution behavior of the rutin nanocrystal-loaded tablet should lead to a better bioavailability of the poorly soluble rutin in the body.     

Enhanced antihypertensive activity of candesartan cilexetil nanosuspension: formulation, characterization and pharmacodynamic study

The objective of the present investigation was to enhance the oral bioavailability of practically insoluble Candesartan cilexetil [CC] by preparing nanosuspension. The nanosuspension was prepared by media milling using zirconium oxide beads and converted to solid state by spray drying. The spray dried nanosuspension of CC [SDCN] was evaluated for particle size, zeta potential, saturation solubility, crystallanity, surface morphology and dissolution behavior. SDCN showed particle size of 223.5±5.4 nm and zeta potential of -32.2±0.6 mV while saturation solubility of bulk CC and SDCN were 125±6.9 μg/ml and 2805±29.5 μg/ml respectively, showing more than 20 times increase in solubility. Differential Scanning Calorimetry [DSC] and X-ray diffraction [XRD] analysis showed that crystalline state of CC remained unchanged in SDCN. Dissolution studies in phosphate buffer pH 6.5 containing 0.7% Tween 20 showed that 53±5% of bulk drug dissolved in 15 min whereas SDCN was almost completely dissolved exhibiting higher dissolution velocity and solubility. Transmission electron microscopy [TEM] revealed that nanocrystals were not of uniform size, and approximately of oval shape. Pharmacodynamic study based on deoxycorticosterone acetate [DOCA] salt model was performed in rats to evaluate in-vivo performance, which showed 26.75±0.33% decrease in systolic blood pressure for nanosuspension while plain drug suspension showed 16.0±0.38% reduction, indicating that increase in dissolution velocity and saturation solubility leads to enhancement of bioavailability of SDCN when compared to bulk CC suspension. Thus, the results conclusively demonstrated a significant enhancement in antihypertensive activity of candesartan when formulated as nanosuspension.     

柚皮素纳米晶体的制备及体外性质研究

目的:制备一种新型的柚皮素纳米晶体并对其进行表征和体外评价。方法:通过高压均质法制备柚皮素纳米结晶;对制备得到的柚皮素纳米晶体进行粒径测定、DSC分析、X-射线衍射分析和傅里叶红外图谱分析,并测定柚皮素纳米晶体的溶解度和体外溶出度。结果:柚皮素纳米晶体的平均粒径为(467±12) nm,DSC、X-射线衍射及傅里叶红外图谱结果表明将柚皮素制备成柚皮素纳米结晶并未改变药物的晶型和化学结构,溶解度和体外溶出度实验结果表明,与柚皮素原料药相比,柚皮素纳米晶体的溶解度和溶出度均有显著地提高。结论:本文通过制备柚皮素纳米晶体,显著地提高了柚皮素的溶解度和体外溶出度,为柚皮素的临床应用提供了新选择。     

伊曲康唑纳米晶体的制备与表征

目的：制备伊曲康唑纳米晶体并进行药剂学性质表征。方法：采用湿法介质研磨结合冷冻干燥工艺制备伊曲康唑纳米晶体;采用马尔文激光粒度测定仪测定伊曲康唑纳米晶体的粒径和多分散系数（PDI）;采用扫描电镜观察伊曲康唑粒子的形态;采用差示扫描量热法、红外光谱法、X-射线粉末衍射法研究伊曲康唑纳米化前后晶型和化学结构变化情况;采用浆法比较伊曲康唑纳米化前后及市售胶囊在pH 1.2、pH 4.0、pH 6.8的溶液以及水等4种溶出介质中的溶出行为。结果：制备的伊曲康唑纳米晶体平均粒径为317 nm,PDI值0.29;纳米化前后伊曲康唑晶型和化学结构没有发生明显改变;在pH 1.2、pH 4.0、pH 6.8的溶液以及水等4种溶出介质中,药物溶出速率快慢顺序为伊曲康唑纳米晶体> 市售伊曲康唑胶囊> 物理混合物及伊曲康唑原料药。结论：采用湿法介质研磨结合冷冻干燥工艺,可以制备平均粒径小且较为均匀的伊曲康唑纳米晶体;纳米化后伊曲康唑仍为结晶态;制成纳米晶体可以明显改善伊曲康唑的溶出性能,利于改善药物的口服吸收。     

葛根素的多晶型研究

目的：解析不同晶态葛根素的理化性质变化。方法：采用4种不同溶剂进行结晶，应用显微放大、溶解度、红外、X射线衍射、热分析。结果：不同晶态的晶体在水中的溶解度随着晶型的增大而减小；热分析显示4种晶体的熔点存在差异；X射线衍射测得4种晶体的厚度不一样，特别是用乙醇水结晶的样品结晶度最低；红外谱图显示4种晶体有差异，并且超临界流体结晶所得样品和标准红外谱图一致。结论：不同晶态的葛根素其理化性质有明显差异。     

Dihydroartemisinin-cyclodextrin complexation: Solubility and stability

Dihydroartemisinin (DHA) is a major metabolite of artemisinin and its derivatives, including arteether, artemether, and artesunate. To improve the solubility and stability of poorly soluble DHA, we prepared inclusion complexes with hydroxypropyl-β-cyclodextrin (HPβCD) and recrystalized DHA to study its thermal stability. The complexes were characterized by differential scanning calorimetery (DSC), Fourier transform infrared spectroscopy (FTIR), X-ray diffraction patterns (XRD), thermal stability, phase, and equilibrium solubility studies. Pure DHA was crystalline and remained crystalline after recrystallization, but its unit cell dimensions changed as exhibited by XRD. DHA-HPβCD complexes showed a phase transitions towards amorphous in DSC thermograms, FTIR spectra, and XRD patterns. The phase solubility profiles of complexes prepared in water, acetate buffer, and phosphate buffers were classified as A_L-type, indicating the formation of a 1:1 stoichiometric inclusion complex. The equilibrium solubility of DHA was enhanced as a function of HPβCD concentration. DHA-HPβCD complexes showed an 89-fold increase in solubility compared to DHA. Solubilities of complexes containing 275.1 mM HPβCD in water, acetate buffer (pH 3.0), and phosphate buffer (pH 3.0 and 7.4) were 10.04, 7.96, 6.30, and 11.61 mg/ml, respectively. Hydrogen bonding was found between DHA and HPβCD, and it was stronger in complexes prepared in water than in buffers. However, the ÄH values were higher in buffer than water. DHA-HPβCD complexes prepared using commercial (untreated) or recrystallized DHA (no detectable impurity) showed a 40% increase in thermal stability (50°C) and a 29-fold decrease in hydrolysis rates compared with DHA. The rank order of stability constants (K_s) was: water, acetate buffer (pH 3.0), phosphate buffer (pH 3.0), and phosphate buffer (pH 7.4). Thus, HPβCD complexation with recrystalized DHA increases DHA solubility and stability.     

Hydrochloride salt co-crystals: preparation,characterization and physicochemical studies

Co-crystallization approach for modification of physicochemical properties of hydrochloride salt is presented. The objective of this investigation was to study the effect of co-crystallization with different co-crystal formers on physicochemical properties of fluoxetine hydrochloride (FH). FH was screened for co-crystallization with a series of carboxylic acid co-formers by slow evaporation method. Photomicrographs and melting points of crystalline phases were determined. The co-crystals were characterized by FTIR, DSC and PXRD methods. Solubility of co-crystals was determined in water and buffer solutions. Powder and intrinsic dissolution profiles were assessed for co-crystals. Physical mixtures of drug and co-formers were used for comparisons at characterizations and physicochemical properties evaluation stages. Four co-crystals of FH viz. Fluoxetine hydrochloride-maleic acid (FH-MA), Fluoxetine hydrochloride-glutaric acid (FH-GA), Fluoxetine hydrochloride-L-tartaric acid (FH-LTA) and Fluoxetine hydrochloride-DL-tartaric acid (FH-DLTA) were obtained from screening experiments. Physical characterization showed that they have unique crystal morphology, thermal, spectroscopic and X-ray diffraction properties. Solubility and dissolution studies showed that Fluoxetine hydrochloride-maleic acid co-crystal possess high aqueous solubility in distilled water, pH 4.6, 7.0 buffer solutions and dissolution rate in distilled water than that of pure drug. Co-crystal formation approach can be used for ionic API to tailor its physical properties.     

Comparison of different methods for preparation of a stable riccardin D formulation via nano-technology

Riccardin D is a new compound extracted from liverwort Marchantia polymorpha L. It has been proved to be useful in antifungal therapy and reversing the resistance of Candida albicans against fluconazole. However, the poor solubility leads to the poor bioavailability and limits its development. In this study, nanocrystals were prepared in the evaporative precipitation into aqueous solution (EPAS) and the microfluidisation process. The characterizations of nanocrystals were compared by transmission electron microscope, size distribution, and zeta potential. In the EPAS method, the drug was dissolved in the organic phase and F68, HPMC, PVP K30 were dissolved in water with the mass ratio of 2:1:2:1. In the microfluidisation process, two key factors - pressure and number of cycles were screened and 8 cycles at 2000 bar was the most efficient parameter. The nanocrystals made in EPAS process were smaller, more uniform and had a narrower distribution than the microfluidisation nanocrystals. Differential scanning calorimetry (DSC) and X-ray diffraction confirmed the crystalline states that were both reserved. The solubility was greatly improved by the two methods and the EPAS nanocrystals were more soluble due to the smaller size. An enhanced dissolution was obvious in vitro. And the stable nanocrystals were successfully achieved by the two methods.     

Bicalutamide nanocrystals with improved oral bioavailability: in vitro and in vivo evaluation

Context: Bicalutamide (BCT) is an antiandrogenic compound belonging to Biopharmaceutics Classification System (BCS) class II drug. Thus it has limited aqueous solubility and hence limited oral bioavailability.

Objective: The purpose of the present investigation was to obtain stable nanocrystals of BCT with improved kinetic solubility, dissolution and pharmacokinetic profiling.

Materials and methods: BCT nanocrystals were prepared by antisolvent precipitation method using Soluplus, a novel amphiphilic polymer. Nanocrystals were characterized for particle size, powder X-ray diffraction analysis (PXRD), in vitro dissolution, in vivo pharmacokinetic profile and stability.

Results and discussion: The obtained nanocrystals had particle size of 168 nm and were spherical in shape. The nanocrystals exhibited fivefold increase in kinetic solubility as compared to pure drug and 85% dissolution in 60 min. PXRD studies established the retention of crystalline polymorphic form II. The in vivo pharmacokinetic study demonstrated that the C_max and AUC of nanosized BCT were about 3.5 times higher as compared to pure drug.

Conclusion: Nanosizing of BCT significantly improved the pharmacokinetic profile of the drug administered to rats. Prepared nanocrystals were found to be stable over the entire stability period. Thus the use of amphiphilic polymer like Soluplus singularly helped in efficient size reduction and stabilization of the drug.     

Preparation and characterization of quercetin nanocrystals

This study is to enhance the dissolution rate of a poorly water-soluble drug, quercetin, by fabricating nanocrystals using high-pressure homogenization. The particle size, crystallinity, dissolution, and antioxidant effects of fabricated quercetin nanocrystals have been investigated. Characterization of the original quercetin powder and nanocrystals was carried out by photon correlation spectroscopy (PCS), laser diffraction, scanning electron microscopy, differential scanning calorimetry (DSC), X-ray diffraction, dissolution tester, and so on. A PCS size of about 483 nm was obtained for the nanocrystals after 20 cycles of homogenization at 1500 bar. X-ray diffraction and DSC studies revealed that the lyophilized quercetin nanoparticles were crystalline after high-pressure homogenization. The percent dissolution efficiency, relative dissolution, mean dissolution time, difference factor (f(1)), and similarity factor (f(2)) were calculated for the statistical analysis. It was found that the dissolution of the drug nanocrystals was much higher than that of the pure drug at pH 6.8 and 1.2. The antioxidant activity and reducing power of the quercetin nanocrystals were more effective than the original quercetin.     

Development of novel itraconazole-loaded solid dispersion without crystalline change with improved bioavailability

To develop a novel itraconazole-loaded solid dispersion without crystalline change with improved bioavailability, various itraconazole-loaded solid dispersions were prepared with water, polyvinylpyrroline, poloxamer and citric acid. The effect of carriers on aqueous solubility of itraconazole was investigated. Their physicochemical properties were investigated using SEM, DSC, and powder X-ray diffraction. The dissolution, bioavailability in rats and stability of solid dispersions were evaluated. Unlike conventional solid dispersion system, the itraconazole-loaded solid dispersion with relatively rough surface did not change crystalline form of drug. Our DSC and powder X-ray diffraction results suggested that this solid dispersion was formed by attaching hydrophilic carriers to the surface of drug without crystal change, resulting in conversion of the hydrophobic drug to hydrophilic form. The itraconazole-loaded solid dispersion at the weight ratio of itraconazole/polyvinylpyrroline/poloxamer of 10/2/0.5 gave maximum drug solubility of about 20 μg/mL. It did not change the crystalline form of drug for at least 6 months, indicating that it was physically stable. It gave higher AUC, C_max and T_max compared to itraconazole powder and similar values to the commercial product, suggesting that it was bioequivalent to commercial product in rats. Thus, it would be useful to deliver a poorly water-soluble itraconazole without crystalline change with improved bioavailability.     

Preparation and Physicochemical Characterization of Acyclovir Cocrystals with Improved Dissolution Properties

Acyclovir is a well-known antiviral agent. It can be administered in very high doses (from 200 to 1000 mg even three-four times daily). It has absorption problems mainly due to its poor solubility in water (about 0.2 g/100 mL at 25°C) and its oral bioavailability is approximately 15%–20% with a half-life of about 3 h. To improve acyclovir solubility and/or its dissolution properties, two cocrystals of this drug were successfully produced with glutaric acid (AGA1:1) and fumaric acid (AFA1:1) as conformers, using a cogrinding method. Their effective formation was investigated by a broad range of techniques: thermal analysis, Fourier transform infrared spectroscopy, X-ray powder diffraction, solid state nuclear magnetic resonance, and scanning electron microscopy coupled with energy dispersive X-ray spectrometry. The water solubility of the AGA1:1 cocrystal was not improved in comparison to acyclovir, while AFA1:1 showed a slight increased solubility at equilibrium. The main difference was detected in terms of intrinsic dissolution rates (IDR). The IDR of the new phases were much faster compared with acyclovir, particularly at neutral pH. AFA1:1 showed the most rapid dissolution behavior in water; within 10 min, the drug was released completely, while just 60% of acyclovir was dissolved in 1 h.     

基于理化性质的枸橼酸托法替布处方前研究

目的 考察枸橼酸托法替布理化性质,为其制剂处方、工艺设计、包装和储藏等提供理论依据。方法 采用HPLC测定药物在不同pH缓冲液及水中的平衡溶解度、脂水分配系数(P)及润湿性;对药物进行影响因素试验;测定药物的粒度、粒度分布、红外光谱(FTIR)、X-射线衍射图谱(XRD)、差示扫描量热图谱(DSC)和扫描电镜图谱(SEM)。结果 枸橼酸托法替布在pH 1.0~8.0的缓冲液及水中的平衡溶解度为0.183 4~22.594 1 mg·mL^-1,属高溶解性药物,其中在pH 1.0缓冲液中的平衡溶解度最大;在上述各介质中,lgP为-1.34~1.28,属低渗透性药物,其中在pH 3.6缓冲液中的lgP最大;在上述各介质中,接触角均<90°,均易于被润湿;枸橼酸托法替布在高温、高湿及强光照射下均较为稳定;平均粒径为(29.85±0.17)µm;XRD、DSC及SEM结果均表明枸橼酸托法替布为结晶性药物,熔点为210 ℃;FTIR结果表明,枸橼酸托法替布在3 375.44,3 134.51,1 732.54,1 711.78,1 625.24,1 551.03,1 529.52,1 473.76,1 448.28,1 409.48,1 348.17,1 213.59,1 170.22,1 115.37,1 077.68,1 023.87,916.97,846.38,775.66,741.84,703.42,603.15,444.07 cm^-1有较强的红外特征峰。结论 枸橼酸托法替布为BCSⅢ类药物,宜设计成胃内滞留型给药系统,有利于药物在上消化道溶解与吸收,以提高生物利用度;本研究使用的枸橼酸托法替布为稳定的结晶性药物,可满足一般制剂生产、包装、贮藏等要求。     

Physical–chemical properties of furosemide nanocrystals developed using rotation revolution mixer

Recently, several approaches have been reported to improve the dissolution rate and bioavailability of furosemide, a class IV drug. However, to the best of our knowledge, none of them proposed nanocrystals. In the last decade, nanocrystals successfully addressed solubility issues by increasing surface area and saturation solubility, both leading to an increase in the dissolution rate of poor water soluble drugs. The preparation of furosemide nanocrystals was by a rotation revolution mixer method. Size distribution and morphology were performed using laser diffraction and scanning electron microscopy, respectively. In addition, differential scanning calorimetry, thermogravimetry, X-ray powder diffraction (XRD) and low frequency shift-Raman spectroscopy allowed investigating the thermal properties and crystalline state. Solubility saturation and intrinsic dissolution rate (IDR) studies were conducted. The thermal analysis revealed lower melting range for the nanocrystals comparing to furosemide. Moreover, a slight crystalline structure change to the amorphous state was observed by XRD and confirmed by low frequency shift Raman. The particle size was reduced to 231?nm with a polydispersity index of 0.232, a 30-fold reduction from the original powder. Finally, the saturation solubility and IDR showed a significant increase. Furosemide nanocrystals showed potential for development of innovative formulations as an alternative to the commercial products.     

芦丁的溶解度及油水分配系数研究

目的研究芦丁在不同介质中的溶解度和油水分配系数,为设计芦丁渗透泵控释制剂提供基础。方法以饱和法测定溶解度,以超声振摇法测定芦丁在正辛醇和水相中的萃取平衡浓度比,计算油水分配系数（P）。结果芦丁在水中的溶解度为194.57mg/L,在2%十二烷基硫酸钠（SDS）溶液中的溶解度为863.17mg/L,在其他不同pH的磷酸盐缓冲溶液中随着pH的升高逐渐升高;油水分配系数随着pH的升高而逐渐降低。结论芦丁为难溶性药物,其溶解度和油水分配系数都与pH有一定的关系;芦丁溶解度和油水分配系数的测定可为进一步研究芦丁渗透泵片提供基础。     

Fabrication of quercetin nanocrystals: Comparison of different methods

The main aim of this study was to prepare quercetin nanocrystals using three fabrication methods, viz. high-pressure homogenization, bead milling, and cavi-precipitation. The three fabrication methods were compared in terms of particle size, saturation solubility, and dissolution of the products obtained. The average particle size of the coarse quercetin was 50.1 μm. The three methods produced quercetin particles in the nanometre range (276-787 nm) and the smallest nanocrystals of around 276.7 nm were fabricated by bead milling. The particle size, polydispersity index, zeta potential, and saturation solubility values for the products fabricated by both high-pressure homogenization and bead mill were similar and thus both represented an efficient means to fabricate quercetin nanosuspensions. According to X-ray diffraction analysis, all nanocrystals were still in the crystalline state after being fabricated by the three methods. The cavi-precipitated product exhibited larger particle size and did not show an optimum stability as suggested by the zeta potential values. However, cavi-precipitated quercetin nanosuspension showed the higher saturation solubility due to the presence of ethanol. The bead milled products with the lowest particle size exhibited a saturation solubility of 25.59 ± 1.11 μg/ml, approximately nine times higher than coarse quercetin. Overall, the dissolution rates of the quercetin nanosuspensions fabricated by these three methods enhanced compared to the coarse quercetin.     

Drug–Drug Coamorphous Systems: Characterization and Physicochemical Properties of Coamorphous Atorvastatin with Carvedilol and Glibenclamide

Purpose

In this study, coamorphous form of atorvastatin calcium (ATC) with two drugs, i.e., carvedilol (CVD) and glibenclamide (GLN) in 1:1 stoichiometry, were prepared from solvent evaporation method and they were characterized and their physicochemical properties determined.

Methods

The coamorphous forms were characterized using differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FT-IR), and powder X-ray diffraction (PXRD). The kinetic solubility of coamorphous form of ATC with CVD (ATC–CVD) and GLN (ATC–GLN) were determined along with stability of supersaturated state of coamorphous forms using developed accurate and precise UV-net analyte signal standard addition method (chemometrics-based approach) and HPLC.

Results

The results of DSC and analysis of glass transition temperatures (T _g), PXRD, and FT-IR indicated that the crystalline studied drugs were converted to coamorphous forms, with unique thermal behaviors, revealing a molecular interaction between two components. The kinetic solubility data revealed that coamorphous forms have better metastable solubility than those of crystalline state. In addition, these systems showed greater solution stability than those for amorphous form of single components reported in the literature.

Conclusion

Coamorphous ATC–CVD and ATC–GLN were shown to have improved physicochemical and solution stability properties as compared to crystalline components.     

Enhanced solubility and bioavailability of flurbiprofen by cycloamylose

The effect of cycloamylose on the aqueous solubility of flurbiprofen was investigated. To improve the solubility and bioavailability of flurbiprofen (poor water solubility), a solid dispersion was spray dried with a solution of flurbiprofen and cycloamylose at a weight ratio of 1:1. The physicochemical properties of solid dispersions were investigated using SEM, DSC, and X-ray diffraction. The dissolution and bioavailability in rats were evaluated compared with a commercial product. Cycloamylose increased solubility of flurbiprofen approximately 12-fold and dissolution of it by 2-fold. Flurbiprofen was present in an unchanged crystalline state, and cycloamylose was a solubilizing agent for flurbiprofen in this solid dispersion. Furthermore, the dispersion gave higher AUC and C_max values compared with the commercial product, indicating that it improved the oral bioavailability of flurbiprofen in rats. Thus, the solid dispersion may be useful to deliver flurbiprofen with enhanced bioavailability without changes in crystalline structure.     

Physicochemical characterization of tacrolimus-loaded solid dispersion with sodium carboxylmethyl cellulose and sodium lauryl sulfate

To develop a novel tacrolimus-loaded solid dispersion with improved solubility, various solid dispersions were prepared with various ratios of water, sodium lauryl sulfate, citric acid and carboxylmethylcellulose-Na using spray drying technique. The physicochemical properties of solid dispersions were investigated using scanning electron microscopy, differential scanning calorimetery and powder X-ray diffraction. Furthermore, their solubility and dissolution were evaluated compared to drug powder. The solid dispersion at the tacrolimus/CMC-Na/sodium lauryl sulfate/citric acid ratio of 3/24/3/0.2 significantly improved the drug solubility and dissolution compared to powder. The scanning electron microscopy result suggested that carriers might be attached to the surface of drug in this solid dispersion. Unlike traditional solid dispersion systems, the crystal form of drug in this solid dispersion could not be converted to amorphous form, which was confirmed by the analysis of DSC and powder X-ray diffraction. Thus, the solid dispersion system with water, sodium lauryl sulfate, citric acid and CMC-Na should be a potential candidate for delivering a poorly water-soluble tacrolimus with enhanced solubility and no convertible crystalline.     

Studies on the preparation, characterization and pharmacokinetics of Amoitone B nanocrystals

Amoitone B, as a new derivative of cytosporone B, has been proved to be a natural agonist for Nur77. It exhibits remarkable anticancer activity in vivo and has the potential to be a therapeutic agent for cancer treatment. However, the poor solubility and dissolution rate result in low therapeutic index for injection and low bioavailability for oral administration, therefore limiting its application. In order to magnify the clinical use of Amoitone B, nanocrystal was selected as an application technology to solve the above problems. In this study, the optimized Amoitone B nanocrystals with small and uniform particle size were successfully prepared by microfluidization method and investigated by morphology, size distribution, and zeta potential. The differential scanning calorimetry (DSC) and X-ray diffraction (XRD) confirmed there was no crystalline state changed in the size reduction process. For Amoitone B nanocrystals, an accelerated dissolution velocity and increased saturation solubility were achieved in vitro and a markedly different pharmacokinetic property in vivo was exhibited with retarded clearance and magnified AUC compared with Amoitone B solution. These results implied that developing Amoitone B as nanocrystals is a promising choice for intravenous delivery and further application for cancer therapy.