Tocophersolan stabilized lipid nanocapsules with high drug loading to improve the permeability and oral bioavailability of curcumin

Bapat, Pradnya; Ghadi, Rohan; Chaudhari, Dasharath; Katiyar, Sameer S.; Jain, Sanyog

doi:10.1016/j.ijpharm.2019.02.013

Cited by 47 publications

(11 citation statements)

References 31 publications

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“…It has high interfacial stability and excellent stability with the payload [ 247 , 248 ]. Such nanosystems have been developed as an effective cancer drug delivery tool to be used via parenteral [ 249 ], topical [ 250 ], or oral routes of administration [ 251 , 252 ].…”

Section: Lipid Based Nanoparticlesmentioning

confidence: 99%

Striking Back against Fungal Infections: The Utilization of Nanosystems for Antifungal Strategies

Gao

Liu

et al. 2021

IJMS

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Fungal infections have become a major health concern, given that invasive infections by Candida, Cryptococcus, and Aspergillus species have led to millions of mortalities. Conventional antifungal drugs including polyenes, echinocandins, azoles, allylamins, and antimetabolites have been used for decades, but their limitations include off-target toxicity, drug-resistance, poor water solubility, low bioavailability, and weak tissue penetration, which cannot be ignored. These drawbacks have led to the emergence of novel antifungal therapies. In this review, we discuss the nanosystems that are currently utilized for drug delivery and the application of antifungal therapies.

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Section: Lipid Based Nanoparticlesmentioning

confidence: 99%

Striking Back against Fungal Infections: The Utilization of Nanosystems for Antifungal Strategies

Gao

Liu

et al. 2021

IJMS

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“…Freeze drying was done using an optimized cycle containing 2.5% w/v and 5% w/v of mannitol and trehalose respectively. All formulations were evaluated after freeze dying for cake appearance, size, as well as entrapment e ciency after re-dispersion [41,42].…”

Section: Freeze Drying Studymentioning

confidence: 99%

Bioavailability Enhancement of Vitamin E TPGS Coated Liposomes of Nintedanib Esylate Formulation Developed Using Quality by Design Approach

Kala

Chinni²

2022

Preprint

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PurposeNintedanib esylate (NE) is a kinase inhibitor designated for the cure of non-small cell lung cancer suffers from first-pass metabolism which resulted in low oral bioavailability (~4.7%). The intent of this exploration was to increase the oral bioavailability of NE by means of TPGS coated liposomes. MethodsThe NE-loaded TPGS coated liposomes were formulated by high-speed homogenization by optimizing process parameters like phospholipids: cholesterol molar ratio, drug loading and sonication time through the design of experiments. The drug's behaviour was studied using a variety of techniques, including physicochemical characterization, in-vitro and in-vivo studies. ResultsThe NE-liposomes had a particle size of 125±6.68 nm, entrapment efficiency of 88.64±4.12% and zeta potential of +46±2.75 mV. X-ray diffraction analysis revealed that NE had been converted to an amorphous state, while transmission electron microscope images showed spherical shape and smooth coating of TPGS on surface of liposomes. The formulation showed Higuchi kinetics with sustained drug release of 88.72 ± 3.40% in 24 hours. Cellular uptake of C-6 labelled liposomes was observed in A-549 cells and cytotoxicity testing revealed that NE-liposomes were more effective than marketed formulation Ofev®. Formulation remained in simulated fluids and for three months in stability chamber and. Liposomal oral bioavailability was ~6.23 times greater in sprague dawley male rats compared to marketed formulation Ofev®, according to in-vivo pharmacokinetic data. ConclusionNE-Liposomal formulations are better for oral administration compared to the marketed capsules because of the prolonged drug release and increased oral bioavailability as a result, the developed formulation can become a successful strategy in cancer chemotherapy.

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“…Nanocapsules have been applied to enhance the oral bioavailability of a wide variety of drugs, including fondaparinux [127], sn-38 [128], paclitaxel [129,130], exenatide [131], tacrolimus [132], psorialidin [133] or furosemide [134], as well as of nutraceuticals, such as curcumin [135], lutein [136] or resveratrol [137,138]. As an example, Peltier et al developed paclitaxel-loaded nanocapsules that were able to enhance the bioavailability of the anti-tumour drug after oral administration to rats.…”

Section: Nanocapsulesmentioning

confidence: 99%

“…: oral; i.v.:intravenous. Adapted with permission of [152] Additional molecules routinely used in the formulation of lipid-based nanocarriers that have shown promise as intestinal Pgp inhibitors include D-α-tocopheryl polyethylene glycol succinate (TPGS) and deoxycholic acid [81,89,135,156]. Vyas et al developed o/w nanoemulsions containing saquinavir that incorporated deoxycholic acid in their aqueous phase.…”

Section: Inhibition Of P-glycoproteinmentioning

confidence: 99%

Current approaches in lipid-based nanocarriers for oral drug delivery

Plaza-Oliver

Santander-Ortega

Lozano

2021

Drug Deliv. and Transl. Res.

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Graphical abstract Lipid-based nanocarriers have gained much interest as carriers of drugs with poor oral bioavailability because of their remarkable advantages like low toxicity, affordable scale-up manufacture, strong biocompatibility or high drug loading efficiency. The potential of these nanocarriers lies in their ability to improve the gastrointestinal stability, solubility and permeability of their cargo drugs. However, achieving efficient oral drug delivery through lipid-based nanocarriers is a challenging task, since they encounter multiple physicochemical barriers along the gastrointestinal tract, e.g. the gastric acidic content, the intestinal mucus layer or the enzymatic degradation, that they must surmount to reach their target. These limitations may be turned into opportunities through a rational design of lipid-based nanocarriers. For that purpose, this review focuses on the main challenges of the oral route indicating the strategies undertaken for lipid-based nanocarriers in order to overcome them. Understanding their shortcomings and identifying their strengths will determine the future clinical success of lipid-based nanocarriers.

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Tocophersolan stabilized lipid nanocapsules with high drug loading to improve the permeability and oral bioavailability of curcumin

Cited by 47 publications

References 31 publications

Striking Back against Fungal Infections: The Utilization of Nanosystems for Antifungal Strategies

Striking Back against Fungal Infections: The Utilization of Nanosystems for Antifungal Strategies

Bioavailability Enhancement of Vitamin E TPGS Coated Liposomes of Nintedanib Esylate Formulation Developed Using Quality by Design Approach

Current approaches in lipid-based nanocarriers for oral drug delivery

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