Microenvironmental pH-modified solid dispersions to enhance the dissolution and bioavailability of poorly water-soluble weakly basic GT0918, a developing anti-prostate cancer drug: Preparation, characterization and evaluation in vivo

Yang, Meiyan; He, Shaolong; Fan, Yunzhou; Wang, Yuli; Ge, Zhenzhong; Li, Shan; Gong, Wenbin; Huang, Xiaoli; Tong, Youzhi; Gao, Chunsheng

doi:10.1016/j.ijpharm.2014.08.047

Cited by 41 publications

(32 citation statements)

References 63 publications

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“…The advantages of SLNs have driven numerous studies with various applications, particularly for parenteral administration of drugs. Typical parenteral SLNs applications include intraarticular to intravenous peroral administration (Muller et al, 2000) increased drug solubility (Yang et al, 2014) and pulmonary delivery (Yang et al, 2012). Studies performed by Gasco et al, revealed that intravenously administered SLNs display prolonged drug plasma levels.…”

Section: Introductionmentioning

confidence: 99%

Delivery of retinoic acid to LNCap human prostate cancer cells using solid lipid nanoparticles

Akanda

Rai

Slipper

et al. 2015

International Journal of Pharmaceutics

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In this study retinoic acid (RTA) loaded solid lipid nanoparticles (SLNs) were optimized by tuning the process parameters (pressure/temperature) and using different lipids to develop nanodispersions with enhanced anticancer activity. The RTA-SLN dispersions were produced by high-pressure homogenization and characterized in terms of particle size, zeta potential, drug entrapment efficiency, stability, transmission electron microscopy (TEM), atomic force microscopy (AFM), X-ray diffraction (XRD) and in vitro drug release. Thermal and X-ray analysis showed the RTA to be in the amorphous state, whilst microscopic images revealed a spherical shape and uniform particle size distribution of the nanoparticles. Anticancer efficiency was evaluated by incubating RTA-SLNs with human prostate cancer (LNCap) cells, which demonstrated reduced cell viability with increased drug concentrations (9.53% at 200 ug/ml) while blank SLNs displayed negligible cytotoxicity. The cellular uptake of SLN showed localization within the cytoplasm of cells and flow cytometry analysis indicated an increase in the fraction of cells expressing early apoptotic markers, suggesting that the RTA loaded SLNs are able to induce apoptosis in LNCap cells. The RTA-SLN dispersions have the potential to be used for prostate anticancer treatment.

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Section: Introductionmentioning

confidence: 99%

Delivery of retinoic acid to LNCap human prostate cancer cells using solid lipid nanoparticles

Akanda

Rai

Slipper

et al. 2015

International Journal of Pharmaceutics

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“…50 PVP is approved by the Food and Drug Administration and is a generally regarded as a safe polymer. 51 It has also been reported that the nanoparticles produced with PVA and PVP improve the correlation between the nanoparticle stability and monomeric length of the polymer chain.…”

Section: Results and Discussion Preparation Of Gefitinib Nanosuspensionmentioning

confidence: 99%

“…As shown in Table 3, CC 50 value of viable cells is nearly 10 times in gefitinib nanosuspension wells as compared to the gefitinib wells. This phenomenon indicates that nanosuspension of gefitinib has low cytotoxicity in comparison with gefitinib.…”

Section: In Vitro Cytotoxicity Studymentioning

confidence: 92%

A quality by design approach on polymeric nanocarrier delivery of gefitinib: formulation, in vitro, and in vivo characterization

Srinivas¹,

Verma

Kulyadi³

et al. 2016

IJN

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“…Fig. 4 shows the color changes by the indicator bromophenol blue (changing range pH 2.8-4.6) for the pHM-SD tablets and the dissolution media at different times, which indicated that an acid environment inside of the tablet was generated (101). To improve the in vitro drug release of weakly acidic AMG009, the alkalify agent was added to the HPMC K100LV matrix, and drug release was improved from less than 4% (5 h) to above 60%.…”

Section: Microenvironment Ph-modified Drug Delivery Systemsmentioning

confidence: 99%

Bioavailability Improvement Strategies for Poorly Water-Soluble Drugs Based on the Supersaturation Mechanism: An Update

Yang¹,

Gong²,

Wang³

et al. 2016

J Pharm Pharm Sci

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-The formulation development for poorly soluble drugs still remains a challenge. Supersaturating drug delivery systems (SDDS) or drug delivery systems based on supersaturating provide a promising way to improve the oral bioavailability of poorly water-soluble drugs. In supersaturable formulations, drug concentration exceeds the equilibrium solubility when exposed to gastrointestinal fluids, and the supersaturation state is maintained long enough to be absorbed, resulting in compromised bioavailability. In this article, the mechanism of generating and maintaining supersaturation and the evaluation methods of supersaturation assays are discussed. Recent advances in different drug delivery systems based on supersaturating are the focus and are discussed in detail.

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Microenvironmental pH-modified solid dispersions to enhance the dissolution and bioavailability of poorly water-soluble weakly basic GT0918, a developing anti-prostate cancer drug: Preparation, characterization and evaluation in vivo

Cited by 41 publications

References 63 publications

Delivery of retinoic acid to LNCap human prostate cancer cells using solid lipid nanoparticles

Delivery of retinoic acid to LNCap human prostate cancer cells using solid lipid nanoparticles

A quality by design approach on polymeric nanocarrier delivery of gefitinib: formulation, in vitro, and in vivo characterization

Bioavailability Improvement Strategies for Poorly Water-Soluble Drugs Based on the Supersaturation Mechanism: An Update

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