Formulation of multifunctional oil-in-water nanosized emulsions for active and passive targeting of drugs to otherwise inaccessible internal organs of the human body

Shunmugaperumal, Tamilvanan

doi:10.1016/j.ijpharm.2009.08.001

Cited by 48 publications

(29 citation statements)

References 122 publications

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“…In the food industry, products have been developed with ingredients that are difficult to absorb, due to their low solubility in water [10]. In the pharmaceutical industry, nanoemulsions can be used for controlled and directed release of drugs [12].…”

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confidence: 99%

Andiroba Oil (Carapa guianensis Aublet) Nanoemulsions: Development and Assessment of Cytotoxicity, Genotoxicity, and Hematotoxicity

Milhomem-Paixão

Fascineli

Muehlmann

et al. 2017

Journal of Nanomaterials

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Andiroba oil (AO) is obtained from an Amazonian plant and is used in traditional medicine. We carried out a comparative study to test the cytotoxicity, genotoxicity, and hematotoxicity of the oil and its nanoemulsion (AN) in vitro (fibroblasts, lineage NIH/3T3) and in vivo (Swiss mice). The AN was characterized by DLS/Zeta, and its stability was investigated for 120 days. The biological activity of AN was assessed in vitro by MTT test and cell morphology analyses and in vivo by micronucleus, comet, and hematotoxicity tests. The AN presented a hydrodynamic diameter (Hd) of 142.5 ± 3.0 and PDI of 0.272 ± 0.007 and good stability at room temperature. The MTT test evidenced the cytotoxicity of AO and of AN only at their highest concentrations, but AN showed lower cytotoxicity than AO. A lower cytotoxicity of AN, when compared to AO, is in fact an interesting data suggesting that during therapeutic application there will be a lower impact in the cell viability of healthy cells. Cytotoxicity, genotoxicity, and hematotoxicity were not observed in vivo. These tests on the biological and toxicological effects of andiroba oil and nanostructured oil are still initial ones but will give a direction to future application in cosmetics and/or the development of new phytotherapics.

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confidence: 99%

Andiroba Oil (Carapa guianensis Aublet) Nanoemulsions: Development and Assessment of Cytotoxicity, Genotoxicity, and Hematotoxicity

Milhomem-Paixão

Fascineli

Muehlmann

et al. 2017

Journal of Nanomaterials

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“…The oil in the MEs influenced the in vivo behavior with CUR DHA ME exhibiting significantly higher C max (maximum concentration), higher area under the curve (AUC) and longer half-life (t 1/2 ) compared to CUR Capmul ME (Table 1). This is attributed to DHA being a long-chain triglyceride, hence exhibiting slow metabolism (Tamilvanan, 2009;Picq et al, 2010;Siddiqui et al, 2013b). The enhancement in plasma AUC compared to CUR solution was 3.79-fold for CUR Capmul ME and a striking 5.74-fold for CUR DHA ME (Figure 2A (a)).…”

Section: Plasma and Brain Pharmacokinetics Following Intravenous Admimentioning

confidence: 96%

Docosahexaenoic acid–mediated, targeted and sustained brain delivery of curcumin microemulsion

Shinde

Devarajan

2017

Drug Delivery

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We disclose microemulsions (ME) of curcumin (CUR) with docosahexaenoic acid (DHA)-rich oil (CUR DHA ME) for targeted delivery to the brain. MEs of CUR (5 mg/mL) with and without DHArich oil (CUR Capmul ME) suitable for intravenous and intranasal administration exhibited negative zeta potential, globule size 520 nm and good stability. Following intravenous delivery MEs exhibited high brain concentration with CUR DHA ME exhibiting a 2.8-fold higher C max than CUR solution. Furthermore, high and sustained concentration was demonstrated even at 24 h, which was 8-and 2-fold higher than CUR solution and CUR Capmul ME, respectively. Brain concentrations following intranasal administration were, however, substantially higher as evident from higher C max and AUC and sustained compared to corresponding intravenous formulations signifying nose to brain targeting. The high brain concentration of CUR DHA ME is ascribed to the targeting efficiency enabled by DHA-mediated transport across the blood-brain barrier (BBB). Histopathological and nasal toxicity confirmed safety of the MEs. Concentrationdependent cytotoxicity in vitro, on human glioblastoma U-87MG cell line was observed with CUR DHA MEs and with the blank DHA ME, implying anticancer potential of DHA. The dramatically low IC 50 value of CUR DHA ME (3.755 ± 0.24 ng/mL) is therefore attributed to the synergistic effect of CUR and DHA in the ME. The CUR concentration achieved with CUR DHA ME at 24 h which translated to 466-fold(intranasal) and 421-fold (intravenous) the IC 50 value in the U-87MG cell line suggests great promise of CUR DHA ME for therapy of brain cancer by both routes.

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“…Enhanced permeability and retention (EPR) effect key: long-circulating drug carriers: (1) penetrate through the leaky pathological vasculature (2) into the tumor interstitium (3) and degrade there, releasing a free drug (4) and creating its high local concentration. Chang & Chu, 2008;Tamilvanan, 2009;Dong et al, 2010;Graziose et al, 2010;Qi et al, 2011).…”

Section: Passive-targeting Tcm Preparationmentioning

confidence: 99%

“…Nevertheless, the size of the emulsion particles has a huge impact on its target distribution. Tamilvanan Shunmugaperumal reviewed the formulation of multifunctional oil-in water nanosized emulsions for active and passive targeting of drugs to otherwise inaccessible internal organs of the human body (Tamilvanan, 2009). In the review, author lists three kinds of generation nanosized emulsions and compares their advantages and disadvantages in pharmacology and clinical applications, respectively.…”

Section: Emulsionmentioning

confidence: 99%

Application of traditional Chinese medicine preparation in targeting drug delivery system

Xing

Dong

et al. 2014

Drug Delivery

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(2015) Application of traditional Chinese medicine preparation in targeting drug delivery system, Drug Delivery, 22:3, 258-265, DOI: 10.3109/10717544.2014 AbstractTargeting drug system (TDS) or targeted drug delivery system (TDDS) is a new kind of drug delivery system which could make drug to be directly concentrated on the target site with high curative effects and low side-effects. As the quintessence of Chinese culture, traditional Chinese medicine (TCM) has a large advantage in many disease clinical treatments, especially in cancer, hypertension and many other intractable diseases owing to their low toxicity and side-effects relative to western medicine. This article reviews literatures on development of TCM-targeted preparations which were published in the past 10 years. TDS including active-targeting, passive-targeting and physical-chemical-targeting preparations were introduced through domestic and overseas literatures to reveal the unique advantages of TCM-targeting preparations in drug delivery system. In this article, we have reviewed some kinds of TCM-targeting preparations and indicated that great attention should be paid to the research on the TCM-targeting preparations.

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Formulation of multifunctional oil-in-water nanosized emulsions for active and passive targeting of drugs to otherwise inaccessible internal organs of the human body

Cited by 48 publications

References 122 publications

Andiroba Oil (Carapa guianensis Aublet) Nanoemulsions: Development and Assessment of Cytotoxicity, Genotoxicity, and Hematotoxicity

Andiroba Oil (Carapa guianensis Aublet) Nanoemulsions: Development and Assessment of Cytotoxicity, Genotoxicity, and Hematotoxicity

Docosahexaenoic acid–mediated, targeted and sustained brain delivery of curcumin microemulsion

Application of traditional Chinese medicine preparation in targeting drug delivery system

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