Bioavailability Enhancement of Paclitaxel via a Novel Oral Drug Delivery System: Paclitaxel-Loaded Glycyrrhizic Acid Micelles

Yang, Fuheng; Zhang, Qing; Liang, Qianying; Wang, Shengqi; Zhao, Boxin; Wang, Ya-Tian; Cai, Yun; Li, Guofeng

doi:10.3390/molecules20034337

Cited by 91 publications

(51 citation statements)

References 45 publications

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“…GA has been reported to have an influence on drug permeation in the skin (Sapra et al, 2008), and it has also been studied as a paclitaxel micelle carrier in our research group (Yang et al, 2015). In the present study, GA's solubilization property improved the solubility of POD and the formulation could reach a concentration of 5 mg/mL.…”

Section: Discussionmentioning

confidence: 49%

“…The preparation of the POD-loaded GA micelles followed the ultrasonic dispersion method (Yang et al, 2015). GA was dissolved in preheated distilled water, and a solution of POD in ethanol was added (the weight ratio of POD: GA was 1:8) dropwise into the preheated aqueous GA solution at 60 C. The resulting solutions contained 5 mg/mL POD, 40 mg/mL GA, and 25% (v/v) ethanol.…”

Section: Preparation Of the Pod-loaded Ga Micellesmentioning

confidence: 99%

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Formulation and evaluation of novel glycyrrhizic acid micelles for transdermal delivery of podophyllotoxin

et al. 2016

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Context: As the first-line agent for genital warts, podophyllotoxin (POD) could induce extensively skin burning, itching, and erythema. Meanwhile, as a common anti-inflammatory agent, glycyrrhizic acid (GA), also has amphipathic and solubilizing properties, indicating that it might be a promising drug carrier.Objective: The objective of this study is to formulate and characterize the POD-loaded GA micelles preparation and to evaluate its drug release characteristics and anti-inflammatory properties. Materials and methods:The novel micelles preparation was prepared by ultrasonic dispersion method and characterized using different scanning calorimetries, dynamic light scattering, and transmission electron microscopies. Subsequently, its encapsulation efficiency (EE), drugloading content (LC), in vitro skin permeation, in vivo drug retention, and distribution of POD were detected. The anti-inflammatory effect of the preparation was reflected by HE staining and immunohistochemistry in the rat skin.Results: The POD-loaded GA micelles formed spherical shapes (approximately 10 nm) with an EE of 78.53 ± 2.17% and a LC of 7.293 ± 0.42%. Meaningfully, unlike the extensive distribution of the POD tincture throughout the skin tissue, POD released from the POD-loaded GA micelles mainly located in the epidermis and could maintain steady skin retention for 12 h. Moreover, the POD-loaded GA micelles induced less leukocyte infiltration and inflammatory factors (IL-6 and TNF-a) expression when compared with the POD tincture. Discussion and conclusion: Our results suggested that the POD-loaded GA micelles could achieve a higher POD distribution in the epidermal layer as well as a lighter skin inflammation. This new POD delivery system might be a potential and promising candidate for genital warts and deserved further researches.

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Section: Discussionmentioning

confidence: 49%

Section: Preparation Of the Pod-loaded Ga Micellesmentioning

confidence: 99%

Formulation and evaluation of novel glycyrrhizic acid micelles for transdermal delivery of podophyllotoxin

et al. 2016

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“…SMA-PTX micelles showed comparable IC 50 values as compared to the free PTX and PTX (Ebewe) in CT-26.luc colon cancer cells. Furthermore, the SMA copolymer did not affect the cell viability at the mentioned concentrations, which is in agreement with the previous study 41 and supports the inert nature of SMA copolymer previously described.…”

mentioning

confidence: 87%

“…49 However, Abraxane, which is an albumin-bound PTX nanoformulation, shows instability in the GI tract 50 and thus is unfavorable for oral administration. Other oral PTX formulations, such as BMS-275183, in a Phase I clinical trial showed grade 1 and grade 2 liver-associated toxicity 51 in four out of 20 patients with nonhematologic malignancy, when administered with an oral dose of 6 mg/m 2 /d of BMS-275183.…”

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confidence: 99%

Styrene maleic acid-encapsulated paclitaxel micelles: antitumor activity and toxicity studies following oral administration in a murine orthotopic colon cancer model

Parayath¹,

Nehoff²,

Norton

et al. 2016

IJN

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Oral administration of paclitaxel (PTX), a broad spectrum anticancer agent, is challenged by its low uptake due to its poor bioavailability, efflux through P-glycoprotein, and gastrointestinal toxicity. We synthesized PTX nanomicelles using poly(styrene-co-maleic acid) (SMA). Oral administration of SMA-PTX micelles doubled the maximum tolerated dose (60 mg/kg vs 30 mg/kg) compared to the commercially available PTX formulation (PTX [Ebewe]). In a murine orthotopic colon cancer model, oral administration of SMA-PTX micelles at doses 30 mg/kg and 60 mg/kg reduced tumor weight by 54% and 69%, respectively, as compared to the control group, while no significant reduction in tumor weight was observed with 30 mg/kg of PTX (Ebewe). In addition, toxicity of PTX was largely reduced by its encapsulation into SMA. Furthermore, examination of the tumors demonstrated a decrease in the number of blood vessels. Thus, oral delivery of SMA-PTX micelles may provide a safe and effective strategy for the treatment of colon cancer.

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“…1,2 It has a significant clinical application for which it is in the World Health Organization's List of Essential Medicines but oral bioavailability of this drug is disgustingly limited by poor water solubility, P-gp efflux and CYP3A metabolism. [3][4][5] Currently, it is administered through intravenous route that is also related to some clinical compromises due to the side effect of used formulation excipients. Several research activities are going on to counteract these situations through different formulation approaches.…”

Section: Introductionmentioning

confidence: 99%

Enhancement of Paclitaxel Oral Bioavailability in Swiss Mice by Four Consecutive Days of Pre-Treatment with Curcumin

Sharma¹,

Magotra²,

Nandi³

et al. 2017

IJPER

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Objective: Poor water solubility, P-glycoprotein (P-gp) efflux property and substrate of CYP3A lead to low oral bioavailability that limit the oral use of paclitaxel, a key anticancer drug. Though several formulation approaches were tried to combat this low absorption profile but effect of pre-treatment with curcumin, a naturally occurring CYP3A and P-gp inhibitor on augmentation of paclitaxel plasma level is not reported till now. Therefore, the objective of the present study is to asses any change in oral pharmacokinetics of paclitaxel. Materials and Methods: curcumin was administered orally to the Swiss mice at a dose of 100 mg/kg for four days and on the fifth day, pharmacokinetics of paclitaxel was carried out at dose of 35 mg/kg orally alone and curcumin pre-treated animals. Results: There is enhancement of Cmax and AUC by 1.4 to 1.5 fold when compared with oral paclitaxel alone treatment that leads to improve in oral bioavailability of paclitaxel. Conclusion: Curcumin can be an ideal candidate for regular use to improve the bioavailability of paclitaxel followed by decrease in dose related side effects. Furthermore, anticancer effect of Curcumin itself as well as with paclitaxel could clinically manage cancer promisingly.

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Bioavailability Enhancement of Paclitaxel via a Novel Oral Drug Delivery System: Paclitaxel-Loaded Glycyrrhizic Acid Micelles

Cited by 91 publications

References 45 publications

Formulation and evaluation of novel glycyrrhizic acid micelles for transdermal delivery of podophyllotoxin

Formulation and evaluation of novel glycyrrhizic acid micelles for transdermal delivery of podophyllotoxin

Styrene maleic acid-encapsulated paclitaxel micelles: antitumor activity and toxicity studies following oral administration in a murine orthotopic colon cancer model

Enhancement of Paclitaxel Oral Bioavailability in Swiss Mice by Four Consecutive Days of Pre-Treatment with Curcumin

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