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Phytonanotechnology
Published in Namrita Lall, Medicinal Plants for Cosmetics, Health and Diseases, 2022
Tafadzwa J. Chiome, Asha Srinivasan
Docetaxel is a well-known semi-synthetic poorly soluble taxane, which is being used in the treatment of breast, lung, oral and prostate cancers. The commercial form of Taxotere is formulated using high concentrations of Tween 80, which is linked to severe side effects like fluid retention, hypersensitivity reaction, mouth sores, hair loss, peripheral neuropathy and nausea (Immordino et al., 2003). Such a formulation resulted in lack of compatibility with poly-vinyl chloride administration sets. As a strategy to overcome multiple drug resistance during the treatment of breast cancer, docetaxel-loaded poly(ε-caprolactone)/Pluronic F68 nanoparticles was shown to be effective when used in docetaxel-resistant human breast cancer cell lines (Harush-Frenkel et al., 2008).
Lutein: A Nutraceutical Nanoconjugate for Human Health
Published in Harishkumar Madhyastha, Durgesh Nandini Chauhan, Nanopharmaceuticals in Regenerative Medicine, 2022
Ishani Bhat, Bangera Sheshappa Mamatha
Mostly, encapsulation systems are emulsion-based, which have core-shelled spheroid lipid droplets distributed in an aqueous medium. Such emulsions generally contain a hydrophobic core (surfactant tails) consisting of lutein and a hydrophilic shell (surfactant head), which makes the emulsion thermodynamically stable. The suspended particles are commonly sized below 100 nm and are called microemulsions. Because hydrophobic drugs are well incorporated into such emulsions within the hydrophobic core, they are commonly used to enhance their oral bioavailability in the pharmaceutical industry. As lutein is also a hydrophobic molecule of biological significance, incorporating it into microemulsions could help improve its oral bioavailability. However, the extent of encapsulation and release from the microemulsion depends on the surfactants, co-surfactants, and oil phases used (Setya et al. 2014; Lo et al. 2016). Tween 80 is a non-ionic food-grade surfactant, which has been successfully used to prepare microemulsions of lutein and zeaxanthin and incorporated into beverages (Amar et al. 2004). A combination of Tween 80, capryol, and transcutol, used to prepare the microemulsion of Rhinacanthusnasutus carotenoid extract by sonication, encapsulated 98.6% of carotenoids (Ho et al. 2016). Besides, the microemulsion exhibited enhanced oral bioavailability (6.25%) in comparison to distilled water suspension.
Designing Smart Nanotherapeutics
Published in Suresh C. Pillai, Yvonne Lang, Toxicity of Nanomaterials, 2019
A. Joseph Nathanael, Tae Hwan Oh, Vignesh Kumaravel
Recently, nano-emulsion-filled alginate hydrogel was fabricated to study the digestion behaviour of hydrophobic nobiletin (3ʹ,4ʹ,5,6,7,8-hexamethoxyflavone) in the gastro intestinal tract (Lei et al. 2017). The nano-emulsion was synthesized by PIT method. Tween 80 and span 20 with a weight ratio of 3:1 were used as surfactants. Medium-chain triglyceride was used as an oil phase. The final formulation of nano-emulsion had 4 g of organic phase, 16 g of aqueous phase, and various amounts of nobiletin (0.0900 g, 0.1200 g, 0.1500 g). The particle size of the nano-emulsion was calculated as 205.3 ± 2.3 nm. Ca2+ cross-linked alginate hydrogel matrix was synthesized using the internal gelling method of calcium carbonate-d-glucono-δ-lactone (CaCO3-GDL) system. The encapsulation of the hydrogel matrix can be beneficial to attain the maximum dissolution and steady release of nobiletin drug from the nano-emulsion. The gelation between Ca2+ and alginate is induced by GDL. Molar ratios of CaCO3 and GDL were 0.5 and 0.135, respectively. The blank hydrogel is transparent in colour with a porous morphology. The nano-emulsion filled hydrogel is milky white in colour. SEM images revealed that the porous structure is completely filled by the nano-emulsion. In vitro experimental studies showed that the bioavailability of nobiletin in the nano-emulsion is higher (67.2 ± 0.4% at 4.5 mg/mL) than that available in the blank (44.7 ± 0.4% at 4.5 mg/mL).
Novel Vitamin E TPGS based docetaxel nanovesicle formulation for its safe and effective parenteral delivery: Toxicological, pharmacokinetic and pharmacodynamic evaluation
Published in Journal of Liposome Research, 2021
Amrinder Singh, Shubham Thakur, Harmanpreet Singh, Harjeet Singh, Sandeep Kaur, Satwinderjeet Kaur, Rajesh Dudi, Dilip Manikrao Mondhe, Subheet Kumar Jain
The present study focuses to eradicate the toxic effects of Tween 80 such as nephrotoxicity, hypersensitivity reactions and fluid retention. Therefore, we hypothesized to formulate Tween 80 free nanocarrier formulations using cholesterol, lipids (either Soya Phosphatidylcholine or Phosphatidylcholine 90-G) and biosurfactants (either Vitamin E TPGS or Sodium Deoxycholate). Table 1 summarized the composition of DTX nanovesicle formulations. Vitamin E TPGS has been selected as a lipid component due to its ability to mix with phospholipids and providing the fluidity to vesicle membranes for better drug loading and encapsulation efficiency. Different formulations were prepared by varying the concentration of Phospholipid and biosurfactants.The amount of drug was fixed in all the formulations to achieve 20 mg/mL strength. To date, no other novel drug delivery system based formulation of DTX in a strength of 20 mg/mL has been reported. During the preparation of nanovesicle, a thin-film hydration method was employed and all the variables such as hydration medium, evaporation time, and the pressure were optimized.
Inhibitory effect of sixteen pharmaceutical excipients on six major organic cation and anion uptake transporters
Published in Xenobiotica, 2021
Ruicong Ma, Gentao Li, Xue Wang, Yajuan Bi, Youcai Zhang
Tween 80 is used in injectable formulations of amiodarone, calcitriol, chlordiazepoxide, docetaxel (substrate of hOATP1B3), doxercalciferol and etoposide (substrate of hOATP1B3), as well as oral formulations of doxycycline, tramadol, and acetaminophen (inhibitor of hOAT1) (Apiwattanakul et al., 1999; Strickley, 2004). The current data suggest that Tween 80 is a strong inhibitor of hOAT3. Tween 80 was reported to inhibit the urinary excretion of methotrexate (Azmin et al., 1985). This might be due to the inhibitory effect of Tween 80 on hOAT3, which has been shown to transport methotrexate with a high affinity (Iwaki et al., 2017). Taxotere, an intravenous drug containing active substance docetaxel, contains 55 mg/kg Tween 80 per dose, leading to a plasma concentration of 550 μg/mL (50 kg adult; 5 liters effective circulating blood volume) (ten Tije et al., 2003). At this concentration, the [I]/IC50 values of Tween 80 for hOCT2, hOAT1, hOAT3, and hOATP1B3 are much higher than 0.1. Thus, the potential Tween 80–drug interactions should be further investigated.
Smart phase transformation system based on lyotropic liquid crystalline@hard capsules for sustained release of hydrophilic and hydrophobic drugs
Published in Drug Delivery, 2020
Xuejuan Zhang, Yujun Xiao, Zhengwei Huang, Jintian Chen, Yingtong Cui, Boyi Niu, Ying Huang, Xin Pan, Chuanbin Wu
As shown in Figure 5(B), the presence of Tween 80 further increased the water uptake of GMO-MLX-PEG 1000 system. While the amount of Tween 80 exhibited no difference in the water uptake profiles. Water uptake with above 45% at 1 h and equilibrium at 6 h were obtained for the Tween 80 incorporated system. As to the drug release profiles, a complete release at 24 h of about 80% MLX were obtained with the presence of Tween 80. Similarly, the amount of Tween 80 exhibited no difference in the drug release profiles. Tween 80, as a nonionic surfactant, has certain irritation due to its damage to cell membrane (Hua et al., 2018). Although it was reported that no obvious toxicity was observed in rats and mice after a long time administration of fodder with 5% Tween 80 (Shah & Paradkar, 2005), 2.5% Tween 80 was chosen for the sake of less probability of toxicity and side effect.