Nanonization of andrographolide by a wet milling method: the effects of vitamin E TPGS and oral bioavailability enhancement

Du, Ping; Jiang, Qikun; Yang, Rujie; Liu, Cuiru; Li, Yingchao; Wang, Liyuan; Xue, Peng; Fu, Qiang; Zhang, Tianhong

doi:10.1039/c6ra16002f

Cited by 9 publications

(3 citation statements)

References 51 publications

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“…TPGS can be used as a stabilizer to fabricate andrographolide nanocrystals. The nanocrystals improved the intestine absorption as evidenced by the single-pass intestinal perfusion studies and oral absorption with significant inhibition on xylene induced ear swelling after oral administration 138 . Moreover, TPGS was applied as stabilizer in fabricating nanocrystals of BCS class Ⅱ drug, telmisartan, with 10-fold increase in bioavailability which was due to the enhanced solubility and dissolution rate 139 .…”

Section: Unmodified Tpgs Based Formulationsmentioning

confidence: 89%

Recent Advances in the Application of Vitamin E TPGS for Drug Delivery

et al. 2018

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D-ɑ-tocopheryl polyethylene glycol succinate (Vitamin E TPGS or TPGS) has been approved by FDA as a safe adjuvant and widely used in drug delivery systems. The biological and physicochemical properties of TPGS provide multiple advantages for its applications in drug delivery like high biocompatibility, enhancement of drug solubility, improvement of drug permeation and selective antitumor activity. Notably, TPGS can inhibit the activity of ATP dependent P-glycoprotein and act as a potent excipient for overcoming multi-drug resistance (MDR) in tumor. In this review, we aim to discuss the recent advances of TPGS in drug delivery including TPGS based prodrugs, nitric oxide donor and polymers, and unmodified TPGS based formulations. These potential applications are focused on enhancing delivery efficiency as well as the therapeutic effect of agents, especially on overcoming MDR of tumors. It also demonstrates that the clinical translation of TPGS based nanomedicines is still faced with many challenges, which requires more detailed study on TPGS properties and based delivery system in the future.

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Section: Unmodified Tpgs Based Formulationsmentioning

confidence: 89%

Recent Advances in the Application of Vitamin E TPGS for Drug Delivery

et al. 2018

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“…The plasma sample preparation was performed according to the previous publication with several modifications [42] . Briefly, 20 µl internal standard (resveratrol, 10 µg/ml) was added into 100 µl plasma samples.…”

Section: Methodsmentioning

confidence: 99%

Integrated computer-aided formulation design: A case study of andrographolide/ cyclodextrin ternary formulation

Gao¹,

Su²,

Wang³

et al. 2021

Asian Journal of Pharmaceutical Sciences

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Current formulation development strongly relies on trial-and-error experiments in the laboratory by pharmaceutical scientists, which is time-consuming, high cost and waste materials. This research aims to integrate various computational tools, including machine learning, molecular dynamic simulation and physiologically based absorption modeling (PBAM), to enhance andrographolide (AG) /cyclodextrins (CDs) formulation design. The lightGBM prediction model we built before was utilized to predict AG/CDs inclusion's binding free energy. AG/γ-CD inclusion complexes showed the strongest binding affinity, which was experimentally validated by the phase solubility study. The molecular dynamic simulation was used to investigate the inclusion mechanism between AG and γ-CD, which was experimentally characterized by DSC, FTIR and NMR techniques. PBAM was applied to simulate the in vivo behavior of the formulations, which were validated by cell and animal experiments. Cell experiments revealed that the presence of D-α-Tocopherol polyethylene glycol succinate (TPGS) significantly increased the intracellular uptake of AG in MDCK-MDR1 cells and the absorptive transport of AG in MDCK-MDR1 monolayers. The relative bioavailability of the AG-CD-TPGS ternary system in rats was increased to 2.6-fold and 1.59-fold compared with crude AG and commercial dropping pills, respectively. In conclusion, this is the first time to integrate various computational tools to develop a new AG-CD-TPGS ternary formulation with significant improvement of aqueous solubility, dissolution rate and bioavailability. The integrated computational tool is a novel and robust methodology to facilitate pharmaceutical formulation design.

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“…6 All these factors directly lead to lower oral bioavailability (2.67%) of AP and seriously limit its pharmacological function. 7 To solve these problems, researchers have designed many new dosage forms for AP such as dispersible tablets, 8 dropping pills, 9 oral microemulsion, 10 liposomes, 11 nanocrystals, 12 and cyclodextrin inclusion complexes. 13 Although desired results were obtained by improving the bioavailability of AP, the clinical application of AP is still restricted because of the lower drug-loading rate, entrapment rate, poor stability of pharmaceutical dosage forms, and the presence of organic solvent residue.…”

Section: Introductionmentioning

confidence: 99%