Long-circulating lipoprotein-mimic nanoparticles for smart intravenous delivery of a practically-insoluble antineoplastic drug: Development, preliminary safety evaluations and preclinical pharmacokinetic studies

Tadros, Mina Ibrahim; Al-mahallawi, Abdulaziz Mohsen

doi:10.1016/j.ijpharm.2015.08.011

Cited by 29 publications

(19 citation statements)

References 44 publications

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“…The protocol of the studies (PI 1738) was evaluated and approved by the Research Ethics Committee in the Faculty of Pharmacy, Cairo University, Egypt. The use and the treatment of animals in all studies were conformed to the EU Directive 2010/63/EU for animal experiments (Tadros & Al-Mahallawi, 2015 ).…”

Section: Methodsmentioning

confidence: 99%

Fabrication of novel elastosomes for boosting the transdermal delivery of diacerein: statistical optimization, ex-vivo permeation, in-vivo skin deposition and pharmacokinetic assessment compared to oral formulation

2018

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Diacerein (DCN) is a hydrophobic osteoarthritis (OA) drug with short half-life and low oral bioavailability. Furthermore, DCN oral administration is associated with diarrhea which represents obstacle against its oral use. Hence, this article aimed at developing elastosomes (edge activator (EA)-based vesicular nanocarriers) as a novel transdermal system for delivering DCN efficiently and avoiding its oral problems. For achieving this goal, elastosomes were prepared according to 41.21 full factorial design using different EAs in varying amounts. The prepared formulae were characterized regarding their entrapment efficiency percentage (EE%), particle size (PS), polydispersity index (PDI), zeta potential (ZP) and deformability index (DI). Desirability function was employed using Design-Expert® software to select the optimal elastosomes (E1) which showed EE% of 96.25 ± 2.19%, PS of 506.35 ± 44.61 nm, PDI of 0.46 ± 0.09, ZP of −38.65 ± 0.91 mV, and DI of 12.74 ± 2.63 g. In addition, E1 was compared to DCN-loaded bilosomes and both vesicles exhibited superior skin permeation potential and retention capacity compared to drug suspension. In-vivo histopathological study was performed which ensured the safety of E1 for topical application. Furthermore, the pharmacokinetic study conducted in albino rabbits demonstrated that there was no significant difference in the rate and extent of DCN absorption from topically applied E1 compared to oral suspension. Multiple level C in-vitro in-vivo correlation showed good correlation between in-vitro release and in-vivo drug performance for E1 and DCN oral suspension. Overall, results confirmed the admirable potential of E1 to be utilized as novel carrier for transdermal delivery of DCN and bypassing its oral side effects.

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Section: Methodsmentioning

confidence: 99%

Fabrication of novel elastosomes for boosting the transdermal delivery of diacerein: statistical optimization, ex-vivo permeation, in-vivo skin deposition and pharmacokinetic assessment compared to oral formulation

2018

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“…As presented in the result of AGN Ex, the fabrication process might influence its amorphization. The amorphization of drug cargos, during the preparation process of injection nanoformulations, was also reported [ 32 , 38 , 39 ]. The interactions between AGN Ex and RSV may play major roles in their loading into the NPs and their sustained release from NPs.…”

Section: Resultsmentioning

confidence: 95%

Development of Resveratrol-Loaded Herbal Extract-Based Nanocomposites and Their Application to the Therapy of Ovarian Cancer

et al. 2018

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Resveratrol (RSV) and the ethanol extract of Angelica gigas Nakai (AGN Ex)-based nanoparticles (NPs) were prepared using the nanocrystal concept. AGN/RSV NPs with 224 nm hydrodynamic size, unimodal size distribution, and negative zeta potential values were developed with the emulsification and solvent evaporation techniques. The crystalline properties of AGN Ex and RSV were transformed during the emulsification and solvent evaporation processes, thus, AGN NPs and AGN/RSV NPs exhibited amorphous states. AGN/RSV NPs held up their initial hydrodynamic size after 24 h of incubation in serum-included media. Sustained release profiles (for 5 days) of decursin (D) and decursinol angelate (DA) (the representative markers of AGN Ex) and RSV were observed at normal physiological pH (pH 7.4). In ovarian cancer (SKOV-3) cells, although AGN/RSV NPs showed a lower cellular entry rate rather than AGN NPs, the cellular accumulated amount of AGN/RSV NPs was similar with that of AGN NPs after 4 h of incubation. The antiproliferation efficiency of AGN/RSV NPs group was significantly higher than the AGN Ex, AGN NPs, and AGN NPs + RSV groups in SKOV-3 cells. AGN/RSV NPs can be one of the promising candidates for therapeutic nanoplatforms against ovarian cancers.

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“…45 At a fixed ethanol%, a direct correlation was revealed between PC concentration and VRD EE%. According to Tadros and Al-mahallawi, 46 this could be explained with respect to the surface-active properties of lecithin which would promote the development of strong coherent layers surrounding the individual vesicles, and thus can minimize the escape of the drug. At a constant system volume, a higher system viscosity would be expected at a higher PC concentration.…”

Section: Resultsmentioning

confidence: 99%

<p>Ethosome-Derived Invasomes as a Potential Transdermal Delivery System for Vardenafil Hydrochloride: Development, Optimization and Application of Physiologically Based Pharmacokinetic Modeling in Adults and Geriatrics</p>

Ammar¹,

Tadros²,

Salama³

et al. 2020

IJN

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Aim The aim of the current work was to develop vardenafil hydrochloride (VRD)-loaded ethosome-derived invasomes as a possible transdermal system which could be used for patients suffering from pulmonary arterial hypertension. Methods VRD-loaded ethosomes were developed at three concentrations of phosphatidylcholine (5, 10 and 15 mg/mL) and three percentages of ethanol (20%, 30% and 40%, v/v). The best achieved VRD-loaded ethosomes (ETH9) were optimized to invasomes via incorporation of terpenes (limonene, cineole and a 1:1 mixture) at three concentrations (0.5%, 1% and 2%, v/v). All systems were evaluated for vesicle size, zeta potential, drug entrapment efficiency (EE%), cumulative drug permeated percentages after 0.5hrs (Q 0.5h ) and 12hrs (Q 12h ) and steady-state flux (J ss ). The optimized system (ETH9-INV8) was further characterized for morphology, histopathology and confocal laser scanning microscopy (CLSM). Physiologically based pharmacokinetic (PBPK) modeling was employed to estimate VRD pharmacokinetic parameters from the optimized transdermal system and an oral aqueous drug dispersion, in adults and geriatrics. Results The optimized invasomal system (ETH9-INV8) was characterized with spherical vesicles (159.9 nm) possessing negative zeta potential (−20.3 mV), promising EE% (81.3%), low Q 0.5h (25.4%), high Q 12h (85.3%) and the largest steady-state flux (6.4 µg.cm −2 h −1 ). Following a leave-on period of 12hrs in rats, it showed minor histopathologic changes. CLSM studies proved its ability to deeply permeate rat skin. Lower C max values, delayed T max estimates and greater AUC 0-24h folds in adults and geriatrics (≈ 2.18 and 1.69, respectively) were estimated following the transdermal application of ETH9-INV8 system. Conclusion ETH9-INV8 is a promising transdermal system for VRD.

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Long-circulating lipoprotein-mimic nanoparticles for smart intravenous delivery of a practically-insoluble antineoplastic drug: Development, preliminary safety evaluations and preclinical pharmacokinetic studies

Cited by 29 publications

References 44 publications

Fabrication of novel elastosomes for boosting the transdermal delivery of diacerein: statistical optimization, ex-vivo permeation, in-vivo skin deposition and pharmacokinetic assessment compared to oral formulation

Fabrication of novel elastosomes for boosting the transdermal delivery of diacerein: statistical optimization, ex-vivo permeation, in-vivo skin deposition and pharmacokinetic assessment compared to oral formulation

Development of Resveratrol-Loaded Herbal Extract-Based Nanocomposites and Their Application to the Therapy of Ovarian Cancer

<p>Ethosome-Derived Invasomes as a Potential Transdermal Delivery System for Vardenafil Hydrochloride: Development, Optimization and Application of Physiologically Based Pharmacokinetic Modeling in Adults and Geriatrics</p>

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