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

Hao, Leilei; Wang, Xiaoyong; Zhang, Dianrui; Xu, Qingyan; Song, Shuai; Wang, Feihu; Li, Caiyun; Guo, Hejian; Liu, Yue; Zheng, Dandan; Qiang, Zhang

doi:10.1016/j.ijpharm.2012.05.002

Cited by 52 publications

(31 citation statements)

References 40 publications

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“…47 Furthermore, the nanometric size of drug particles may decrease the thickness of the diffusion layer between the surface of particle and bulk solution leading to an increase in the dissolution velocity, which could be explained by the Prandtl equation. 21 This was in a good agreement with the previous results that confirm the choice of RIF NS (F 5 ) containing 0.4% w/v PVA as an optimum NS formulation for further characterization.…”

supporting

confidence: 91%

“…The result could be contended with the Ostwald-Freundlich equation, which revealed that the improvement of drug solubility depends on its particle size. 13 Hao et al 21 reported that Amoitone B nanocrystals showed a three-and 15-fold increase in drug solubility in comparison to its physical mixture with Pluronic F68 and powder, respectively, due to the difference in particle size. As implied in Table 3, the particle size of the RIF nanocrystals (F 5 ) (101.7 nm) was smaller than that of Amoitone B nanocrystals (256.3 nm).…”

Section: Rif Solubility Determinationmentioning

confidence: 99%

“…18 This technology is a popular approach used for its simplicity and low setup cost. 18 It has been widely reported in many studies for preparing different drug nanocarriers as nitrendipine, 19 quercetin, 20 amoitone B, 21 and camptothecin. 22 Realizing the obstacles of RIF, the impact of NS on enhancing its water solubility as well as dissolution characteristics will be a field of interest.…”

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confidence: 99%

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The relevancy of controlled nanocrystallization on rifampicin characteristics and cytotoxicity

Mohyeldin

Mehanna

Elgindy

2016

IJN

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Purpose This article investigated the influence of novel rifampicin nanosuspension (RIF NS) for enhancing drug delivery properties. Methods RIF NS was fabricated using the antisolvent precipitation technique. The impact of solvent type and flow rate, stabilizer type and concentration, and stirring time and apparatus together with the solvent–antisolvent volume ratio on its controlled nanocrystallization has been evaluated. NSs were characterized by transmission electron microscopy, particle size and zeta potential analysis, solubility, and dissolution profiles. The compatibility between RIF and the stabilizer was investigated via Fourier transform infrared spectroscopy and the differential scanning calorimetry techniques. The shelf-life stability of the RIF NS was assessed within a period of 3 months at different storage temperatures. Cell cytotoxicity was evaluated using 3(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay on lung epithelial cells. Results Polyvinyl alcohol at 0.4% w/v, 1:15 methanol to deionized water volume ratio and 30-minutes sonication were the optimal parameters for RIF NS preparation. Nanocrystals were obtained with a nanometeric particle size (101 nm) and a negative zeta potential (−26 mV). NS exhibited a 50-fold enhancement in RIF solubility and 97% of RIF was dissolved after 10 minutes. The RIF NS was stable at 4±0.5°C with no significant change in particle size or zeta potential. The MTT cytotoxicity assay of RIF NS demonstrated a good safety profile and reduction in cell cytotoxicity with half maximal inhibitory concentration values of 0.5 and 0.8 mg/mL for free RIF and RIF NS, respectively. Conclusion A novel RIF NS could be followed as an approach for enhancing RIF physicochemical characteristics with a prominence of a safer and better drug delivery.

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confidence: 91%

Section: Rif Solubility Determinationmentioning

confidence: 99%

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confidence: 99%

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The relevancy of controlled nanocrystallization on rifampicin characteristics and cytotoxicity

Mohyeldin

Mehanna

Elgindy

2016

IJN

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“…35,36 Moreover, the crystalline state is a factor affecting the dissolution rate and physical stability of the nanocrystal suspensions. 37 Thus, before and after the nanosizing process, XRPD study was carried out to evaluate if the initial crystalline state was preserved. …”

Section: 31mentioning

confidence: 99%

In vitro and in vivo evaluation of SN-38 nanocrystals with different particle sizes

Chen¹,

Li²,

Zhang³

et al. 2017

IJN

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7-Ethyl-10-hydroxycamptothecin (SN-38) is a potent broad-spectrum antitumor drug derived from irinotecan hydrochloride (CPT-11). Due to its poor solubility and instability of the active lactone ring, its clinical use is significantly limited. As one of the most promising formulations for poorly water-soluble drugs, nanocrystals have attracted increasing attention. In order to solve these problems and evaluate the antitumor effect of SN-38 in vitro and in vivo, two nanocrystals with markedly different particle sizes were prepared. Dynamic light scattering and transmission electron microscopy were used to investigate the two nanocrystals. The particle sizes of SN-38 nanocrystals A (SN-38/NCs-A) and SN-38 nanocrystals B (SN-38/NCs-B) were 229.5±1.99 and 799.2±14.44 nm, respectively. X-ray powder diffraction analysis showed that the crystalline state of SN-38 did not change in the size reduction process. An accelerated dissolution velocity of SN-38 was achieved by nanocrystals, and release rate of SN-38/NCs-A was significantly faster than that of SN-38/NCs-B. Cellular uptake, cellular cytotoxicity, pharmacokinetics, animal antitumor efficacy, and tissue distribution were subsequently examined. As a result, enhanced intracellular accumulation in HT1080 cells and cytotoxicity on different tumor cells were observed for SN-38/NCs-A compared to that for SN-38/NCs-B and solution. Besides, compared to the SN-38 solution, SN-38/NCs-A had a higher bioavailability after intravenous injection; while the bioavailability of SN-38/NCs-B was even lower than that of the SN-38 solution. SN-38/NCs-A exhibited a significant inhibition of tumor growth compared to SN-38 solution and SN-38/NCs-B in vivo. The antitumor effect of SN-38/NCs-B was stronger than SN-38 solution. The tissue distribution study in tumor-bearing mice showed that nanocrystals could markedly improve the drug accumulation in tumor tissue by the enhanced permeability and retention effect compared to SN-38 solution, and the amount of SN-38 in tumors of SN-38/NCs-A group was much more than that of SN-38/NCs-B group. In conclusion, nanocrystals dramatically enhanced the anticancer efficacy of SN-38 in vitro and in vivo, and the particle size had a significant influence on the dissolution behavior, pharmacokinetic properties, and tumor inhibition of nanocrystals.

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“…However, the waterinsolubility and short biological half-time restrict its successful application. In order to improve the dissolution velocity and saturation solubility, nanocrystal technology was investigated (Hao et al, 2012), but there has no research about colloidal drug carriers so far.…”

Section: Introductionmentioning

confidence: 99%

Design and characterization of Amoitone B-loaded nanostructured lipid carriers for controlled drug release

et al. 2013

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Amoitone B, a novel compound chemically synthesized as the analogue of cytosporone B, has been proved to own superior affinity with Nur77 than its parent compound and exhibit notable anticancer activity. However, its application is seriously restricted due to the water-insolubility and short biological half-time. The aim of this study was to construct an effective delivery system for Amoitone B to realize sustained release, thus prolong drug circulation time in body and improve the bioavailability. Nanostructured lipid carriers (NLC) act as a new type of colloidal drug delivery system, which offer the advantages of improved drug loading and sustained release. Amoitone B-loaded NLC (AmB-NLC) containing glyceryl monostearate (GMS) and various amounts of medium chain triglycerides (MCT) were successfully prepared by emulsion-evaporation and low temperature-solidification technology with a particle size of about 200 nm and a zeta potential value of about À20 mV. The results of X-ray diffraction and DSC analysis showed amorphous crystalline state of Amoitone B in NLC. Furthermore, the drug entrapment efficacy (EE) was improved compared with solid lipid nanoparticles (SLN). The EE range was from 71.1% to 84.7%, enhanced with the increase of liquid lipid. In vitro drug release studies revealed biphasic drug release patterns with burst release initially and prolonged release afterwards and the release was accelerated with augment of liquid lipid. These results demonstrated that AmB-NLC could be a promising delivery system to control drug release and improve loading capacity, thus prolong drug action time in body and enhance the bioavailability.

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

Cited by 52 publications

References 40 publications

The relevancy of controlled nanocrystallization on rifampicin characteristics and cytotoxicity

The relevancy of controlled nanocrystallization on rifampicin characteristics and cytotoxicity

In vitro and in vivo evaluation of SN-38 nanocrystals with different particle sizes

Design and characterization of Amoitone B-loaded nanostructured lipid carriers for controlled drug release

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