Enhanced oral bioavailability of piperine by self-emulsifying drug delivery systems:<i>in vitro, in vivo</i>and<i>in situ</i>intestinal permeability studies

Lei, Lei; Cui, Chao; Ji, Hongyu; Tang, Jingling; Wang, Zhiyong; Li, Hongmei; Qin, Mengnan; Li, Xin; Lin-hua, WU

doi:10.3109/10717544.2014.898109

Cited by 82 publications

(54 citation statements)

References 34 publications

(37 reference statements)

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“…The rats were divided into different groups at random before the experiments. The surgical procedure for the single-pass intestinal perfusion experiments was performed as previously described15, 25. The process was as follows: the rats were anesthetized with an intraperitoneal injection of sodium pentobarbital.…”

Section: Methodsmentioning

confidence: 99%

Self-microemulsifying drug delivery system for improving the bioavailability of huperzine A by lymphatic uptake

Wang

et al. 2017

Acta Pharmaceutica Sinica B

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Huperzine A (Hup-A) is a poorly water-soluble drug with low oral bioavailability. A self-microemulsifying drug delivery system (SMEDDS) was used to enhance the oral bioavailability and lymphatic uptake and transport of Hup-A. A single-pass intestinal perfusion (SPIP) technique and a chylomicron flow-blocking approach were used to study its intestinal absorption, mesenteric lymph node distribution and intestinal lymphatic uptake. The value of the area under the plasma concentration–time curve (AUC) of Hup-A SMEDDS was significantly higher than that of a Hup-A suspension (P<0.01). The absorption rate constant (Ka) and the apparent permeability coefficient (Papp) for Hup-A in different parts of the intestine suggested a passive transport mechanism, and the values of Ka and Papp of Hup-A SMEDDS in the ileum were much higher than those in other intestinal segments. The determination of Hup-A concentration in mesenteric lymph nodes can be used to explain the intestinal lymphatic absorption of Hup-A SMEDDS. For Hup-A SMEDDS, the values of AUC and maximum plasma concentration (Cmax) of the blocking model were significantly lower than those of the control model (P<0.05). The proportion of lymphatic transport of Hup-A SMEDDS and Hup-A suspension were about 40% and 5%, respectively, suggesting that SMEDDS can significantly improve the intestinal lymphatic uptake and transport of Hup-A.

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Section: Methodsmentioning

confidence: 99%

Self-microemulsifying drug delivery system for improving the bioavailability of huperzine A by lymphatic uptake

Wang

et al. 2017

Acta Pharmaceutica Sinica B

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“…In addition, capsaicin-loaded microemulsion and liposomal nanoformulation both enhanced oral bioavailability [264,265,266,267]. As for piperine, a self-emulsifying drug delivery system could enhance oral bioavailability of piperine [268]. …”

Section: Bioavailability Of Active Compounds From Spicesmentioning

confidence: 99%

Spices for Prevention and Treatment of Cancers

et al. 2016

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Spices have been widely used as food flavorings and folk medicines for thousands of years. Numerous studies have documented the antioxidant, anti-inflammatory and immunomodulatory effects of spices, which might be related to prevention and treatment of several cancers, including lung, liver, breast, stomach, colorectum, cervix, and prostate cancers. Several spices are potential sources for prevention and treatment of cancers, such as Curcuma longa (tumeric), Nigella sativa (black cumin), Zingiber officinale (ginger), Allium sativum (garlic), Crocus sativus (saffron), Piper nigrum (black pepper) and Capsicum annum (chili pepper), which contained several important bioactive compounds, such as curcumin, thymoquinone, piperine and capsaicin. The main mechanisms of action include inducing apoptosis, inhibiting proliferation, migration and invasion of tumors, and sensitizing tumors to radiotherapy and chemotherapy. This review summarized recent studies on some spices for prevention and treatment of cancers, and special attention was paid to bioactive components and mechanisms of action.

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“…Piperine was released relatively quickly in the first three hours to obtain about 60% and gradually released until completed (102.69 ± 17.02%) at 12 h. This is because piperine had relatively high solubility (0.164 mg/mL) [37] compared with curcumin (0.6 µg/mL) [36], and the lower layer containing piperine directly contacted the buffer in the receptor phase of the modified Franz diffusion cell. The rapid and complete release of piperine from the composite membrane would be benefited via interaction with the skin structure before curcumin would be delivered through the skin.…”

Section: Release Studymentioning

confidence: 99%

Effect of Piperine on Skin Permeation of Curcumin from a Bacterially Derived Cellulose-Composite Double-Layer Membrane for Transdermal Curcumin Delivery

et al. 2018

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Curcumin is a naturally occurring substance with various pharmacological activities. It has not been developed as a drug because of its low bioavailability due to its low solubility and absorption. Piperine is a natural enhancer that is popularly used to increase the absorption of curcumin in oral applications; however, it has not been applied for transdermal curcumin delivery. This study aims to develop a transdermal curcumin delivery system using piperine as a skin permeation enhancer in the form of composite double-layer membrane; the upper layer consisted of curcumin and the lower layer consisted of piperine. The amount of curcumin was fixed, but the amount of piperine varied at three levels from 1.96% to 7.41%. The composite membrane had moderate mechanical strength (15⁻22 MPa) with a good swelling degree (~435%). From an in vitro skin permeation study, piperine had the effect to increase the permeation of curcumin. The permeation rate was related to the amount of piperine. The composite membrane containing piperine at 7.41% could increase the permeation rate of curcumin by about 1.89 times compared with non-piperine contained membrane. Bacterially-derived cellulose containing curcumin and piperine may have the potential for transdermal curcumin delivery in order to improve curcumin's bioavailability.

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Enhanced oral bioavailability of piperine by self-emulsifying drug delivery systems:in vitro, in vivoandin situintestinal permeability studies

Cited by 82 publications

References 34 publications

Self-microemulsifying drug delivery system for improving the bioavailability of huperzine A by lymphatic uptake

Self-microemulsifying drug delivery system for improving the bioavailability of huperzine A by lymphatic uptake

Spices for Prevention and Treatment of Cancers

Effect of Piperine on Skin Permeation of Curcumin from a Bacterially Derived Cellulose-Composite Double-Layer Membrane for Transdermal Curcumin Delivery

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