Solid lipid nanoparticles as delivery systems for Gambogenic acid

Huang, Xia; Chen, Yanjie; Peng, Daiyin; Li, Qinglin; Wang, Xiaoshan; Wang, Dianlei; Chen, Weidong

doi:10.1016/j.colsurfb.2012.08.058

Cited by 54 publications

(47 citation statements)

References 32 publications

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“…Figure 10 illustrated that the double peaks of maximum concentrations were observed for GNA solution, which may be attributed to the enterohepatic circulation. This was in accordance with the previous study of Huang et al (Huang et al, 2013). However, there was no double peaks phenomenon in rats by administration of GNA-NS.…”

Section: In Vivo Evaluation Of Gna-nssupporting

confidence: 93%

“…However, the poor solubility, short biological half-life and excessive vascular irritation of GNA hindered its clinical application (Hua et al, 2015). In order to enhance delivery efficiency and bioavailability of GNA, we have used nanotechnology and successfully prepared PEGylated non-ionic surfactant vesicles and solid lipid nanoparticles of GNA in previous researches (Huang et al, 2013;Lin et al, 2013). Nevertheless, low drug encapsulation efficiency and drug loading, residual organic solvent, especially a large amount of excipients and surfactants used in these nano-carriers will cause many side effects, such as toxicity and hemolysis.…”

Section: Introductionmentioning

confidence: 99%

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Nanosuspensions as delivery system for gambogenic acid: characterization and in vitro/in vivo evaluation

Yuan

Zhang

et al. 2015

Drug Delivery

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Nanosuspensions (NS) can enhance the saturation solubility and dissolution velocity of poorly soluble drugs. PEG as a non-ionic surfactant plays an important role in surface modification of nanoparticles for prolonging in vivo circulation. In this study, anti-solvent precipitation method was introduced to prepare gambogenic acid nanosuspensions (GNA-NS) with PVPK30 and PEG2000 as stabilizers to settle the disadvantages of GNA. The obtained nanoparticles were spherical with a mean particle size of 183.7 nm and a zeta potential of À22.8 mV.The entrapment efficiency and drug loading of the resultant formulation were 97.3 and 29.73%. X-ray diffraction analysis confirmed the amorphous phase of GNA in NS. Fourier transform infrared indicated there may be hydrogen bond interaction between the drug and excipients. After lyophilization of GNA-NS, the freeze-dried powder displayed sufficient longterm physical stability at 4 and 25 C. In comparison to GNA solution, in vitro studies of GNA-NS showed much slower release and higher cytotoxicity in HepG2 cells. What's more, the pharmacokinetic study in rats revealed that the AUC 0-1 and t 1/2 of GNA-NS were increased 2.63-and 1.77-fold than that of the reference formulation. Taken together, in vitro/in vivo evaluations showed NS would be an effectively strategy to change the poor aqueous solubility and prolong the half-life for GNA. The GNA-NS with enhanced bioavailability and drug efficacy provided a promising delivery system for the application of GNA. KeywordsCytotoxicity, gambogenic acid, in vivo pharmacokinetics, in vitro release, nanosuspensions History

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Section: In Vivo Evaluation Of Gna-nssupporting

confidence: 93%

Section: Introductionmentioning

confidence: 99%

Nanosuspensions as delivery system for gambogenic acid: characterization and in vitro/in vivo evaluation

Yuan

Zhang

et al. 2015

Drug Delivery

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“…The samples were assayed for GNA using the HPLC method reported earlier (Huang et al, 2013). HPLC was equipped with Shimadzu LC-15C, SPD-15 C UV-Spectrophotometric detector.…”

Section: Hplc Analysis Of Gnamentioning

confidence: 99%

“…It is because that the colloidal particulate carriers have distinct advantages over conventional carriers forms not only for their inherent associated adjuvanticity, but also for the particles which can act as drug containing reservoirs (Abd-Elbaty et al, 2008;Manosroi et al, 2008;Hong et al, 2009;Aburahma & Abdelbary, 2012). From this point of view, we have successfully prepared highly stable solid lipid nanoparticles for Gambogenic acid (GNA-SLNs) in our previous studies (Huang et al, 2013). The GNA-SLNs effectively reduced toxicity of the free drug, while the materials of GNA-SLNs are high in cost, which are not so economically possible in the industrial production.…”

Section: Introductionmentioning

confidence: 99%

PEGylated non-ionic surfactant vesicles as drug delivery systems for Gambogenic acid

et al. 2013

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Gambogenic acid (GNA), a popular Chinese traditional medicine, has its limitations of coming into use due to its low aqueous solubility and poor bioavailability. In this study, therefore, the PEGylated non-ionic surfactant vesicles drug delivery systems were prepared from biocompatible non-ionic surfactant of Span60, cholesterol and dicetyl phosphate (DCP) by the improved ethanol injection method, and were modified with a polyethylene glycol monostearate15 (PEG15-SA). PEG15-SA, as a biocompatible, non-toxic and non-immunogenic hydrophilic segment, was grafted onto the surface of colloidal niosomes carries to reduce the uptake by the reticuloendothelial system (RES), prolonging the circulation time and attaining higher entrapment efficiency. To our knowledge, this work is the first to report that PEG15-SA was applied to coating of niosomes for encapsulation of GNA. The optimized PEG-GNA-NISVs (P-GNA-NISVs) were characterized in terms of mean vesicles size, polydispersity index (PDI), Zeta potential and entrapment efficiency of the P-GNA-NISVs. The results showed that the mean diameter, PDI, Zeta potential, and the entrapment efficiency of the P-GNA-NISVs were 70.1 nm, 0.166, À44.3 mV and 87.74%, respectively. Furthermore, the release studies of GNA from PEGylated niosomes in vitro and the pharmacokinetics in vivo exhibited a prolonged release profile as studied over 24 h. In conclusion, the result suggests that P-GNA-NISVs prepared in this way not only have higher encapsulation capacity, more colloidal stability but also offer an approach that the PEGylated niosomes is a promising carrier for anticancer GNA.

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“…Compared to traditional carriers, SLN had several advantages, such as good biocompatibility, controlled drug release and improved solubility of drug (Mehnert & Mader, 2001). In recent years, much works have been focused on the preparation of SLN of poor water-soluble drugs for improving bioavailability (Chirio et al, 2011;Bhandari & Kaur, 2013;Huang et al, 2013). Nonetheless, there were also some limitations of the SLN system, such as limited drug loading capacity due to the solubility of the drug in the solid lipid and drug expulsion during storage (when lipid crystallizes to the stable b-form) (Chinsriwongkul et al, 2011).…”

Section: Introductionmentioning

confidence: 99%

Nanostructured lipid carriers as a delivery system of biochanin A

Wang¹,

Cheng²,

Zhou³

et al. 2013

Drug Delivery

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The aim of this study was to explore the nanostructured lipid carriers as a delivery system of biochanin A so as to supply a method to improve its bioavailability. Biochanin A-loaded nanostructured lipid carriers (BCA-NLCs) were prepared by the method of emulsionevaporation and low temperature solidification. Pharmacokinetics was carried out in rats upon oral administration at a dose of 10 mg/kg. BCA-NLC showed spherical formulation and had mean diameter174.68 AE 0.96 nm, zeta potential À20.9 AE 0.8 mv and entrapment efficiency 97.36 AE 0.14%. DSC and XRD studies indicated that BCA was not in crystal state in NLC. In in vitro release study, the BCA from BCA-NLC exhibited a biphasic release pattern with burst release initially and sustained release afterwards. BCA-NLC showed higher AUC value and circulated in blood for a longer time than BCA suspension. The studies demonstrated that NLC could be a potential delivery system for BCA to improve bioavailability.

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Solid lipid nanoparticles as delivery systems for Gambogenic acid

Cited by 54 publications

References 32 publications

Nanosuspensions as delivery system for gambogenic acid: characterization and in vitro/in vivo evaluation

Nanosuspensions as delivery system for gambogenic acid: characterization and in vitro/in vivo evaluation

PEGylated non-ionic surfactant vesicles as drug delivery systems for Gambogenic acid

Nanostructured lipid carriers as a delivery system of biochanin A

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