Improved Oral Bioavalability of Mebudipine Upon Administration in PhytoSolve and Phosal-Based Formulation (PBF)

Khani, Samira; Keyhanfar, Fariborz

doi:10.1208/s12249-013-0039-x

Cited by 10 publications

(10 citation statements)

References 16 publications

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“…[24])—and NAPC to enhance the oral bioavailability of the poorly water‐soluble calcium channel blocker mebudipine in rats. [ 25 ] The optimized NAPC contained PHOSAL 50 PG/glycerol in a 6/4 ratio (w/w). PhytoSolve and the NAPC were miscible with water in any ratio and did not demonstrate any phase separation or drug precipitation over 1 month of storage.…”

Section: Resultsmentioning

confidence: 99%

Non‐Aqueous Phospholipid Concentrates for Increasing the Bioavailability of Poorly Soluble Compounds

Hoogevest

2020

Euro J Lipid Sci & Tech

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The properties and use of liquid non-aqueous phospholipid concentrates (NAPC) are reviewed. They are mainly used to solubilize poorly water-soluble drug substances to enhance their oral bioavailability, but they also find applicability in dietetics and cosmetics. Due to the large-scale availability of these concentrates at good manufacturing practice quality including Drug Master File (DMF) documentation, they can be used for pre-clinical screening and clinical testing and as market form, as demonstrated by the product of Wyeth/Pfizer, Rapamune, enabling a cost effective and fast dosage form development. When needed, NAPC can be converted to solid dosage forms by means of a capsule fill or addition of adsorbing excipients. It is concluded that NAPC deserve more attention and a broader use in the life science industry. Practical Applications: NAPCs are suitable as pre-clinical formulation vehicle for screening of the oral bioavailability of poorly water-soluble compounds. The same formulation can be used for clinical testing and market introduction, allowing a fast track dosage form development. When needed NAPC can be converted to solid dosage forms. NAPC have also applicability in dietetics and cosmetics to solubilize poorly water-soluble compounds.

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Section: Resultsmentioning

confidence: 99%

Non‐Aqueous Phospholipid Concentrates for Increasing the Bioavailability of Poorly Soluble Compounds

Hoogevest

2020

Euro J Lipid Sci & Tech

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“…For each of the variables, the range was determined, aiming not only to study its influence on the considered responses but also to include all of the conditions which were possible within the formulation process to develop lipidic nanocarriers devoid of any physical stability problems, including aggregation, fusion, and sedimentation (Table S1 in the Supporting Information). With regard to previous reports (Keyhanfar et al., ; Khani & Keyhanfar, ), we first assessed physicochemical properties of the vesicles prepared at varying concentrations of total lipid and CoQ10 using EPC to MCT weight ratio of 1:4 and 50% glycerol aqueous solution. Regarding the preliminary findings, it was revealed that increasing the concentrations of total lipid from 50 to 100 mg/g and CoQ10 from 5 to 15 mg/g led to the development of more monodisperse vehicles with smaller particle size (91 nm) and acceptable entrapment (∼66%), but further increasing the concentration of CoQ10 (20 mg/g) caused instability of the formulations (Table S1 in the Supporting Information).…”

Section: Resultsmentioning

confidence: 99%

“…The proposed nanocarriers are composed of an oily phase (MCT), where the lipophilic cargo could be dissolved, stabilized by phospholipid molecules (EPC) to disperse within an aqueous solution of carbohydrate or polyol. The presence of a polyol or carbohydrate in the aqueous phase leads to the reduction of interfacial tension between the dispersed and continuous phases, resulting in the formation of monodisperse particles with a smaller diameter size (Khani & Keyhanfar, ).…”

Section: Discussionmentioning

confidence: 99%

“…Among the recent efforts in this regard are triglyceride/phospholipid‐based nanocarriers, which have been proposed to improve the solubility of lipophilic molecules (Keyhanfar, Khani, & Bohlooli, ; Khani & Keyhanfar, ). These nanocarriers are capable of fulfilling the main prerequisites, which are required for a novel formulation, aimed at being introduced into the pharmaceutical market, such as accepted status of excipients, simplicity of the formulation process, low production cost, and large‐scale production facilities.…”

Section: Introductionmentioning

confidence: 99%

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Green Formulation of Triglyceride/Phospholipid‐Based Nanocarriers as a Novel Vehicle for Oral Coenzyme Q10 Delivery

Alavi

Akhlaghi

Dadashzadeh

et al. 2019

Journal of Food Science

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This study was aimed to develop a novel nanocarrier for coenzyme Q10 (CoQ10) by a green process that prevented the use of surfactants and organic solvents. Triglyceride/phospholipid‐based nanocarriers were developed through high‐pressure homogenization (an industrial feasible process), and a 25‐1 fractional factorial design was adopted to assess the influences of formulation variables on the considered responses, including vesicle size, entrapment efficiency, loading capacity, and solubility of the vehicles in simulated gastrointestinal fluids. The optimized formulation was further in‐depth characterized in terms of morphology, release behavior, biocompatibility (Caco‐2 cell cytotoxicity and histological examination), thermal behavior, and Fourier transform infrared analysis. Optimal nanocarriers were found to have mean particle size of 75 nm, narrow particle distribution, and CoQ10 entrapment of 95%. The optimized formulation was stable upon incubation in simulated gastrointestinal fluids without considerable leakage of cargo, which was in agreement with their sustained release behavior. Microscopic observations also confirmed nanosized nature of the vesicles and revealed their spherical shape. Moreover, toxicity evaluations at the cellular and tissue levels revealed their nontoxic nature. In conclusion, triglyceride/phospholipid‐based nanocarriers proved to be a green safe vehicle for delivery of CoQ10 with industrial‐scale production capability and could provide a new horizon for delivery of hydrophobic nutraceuticals. Practical application Green nanostructure formulation approaches have recently gained tremendous attraction for their safe profile especially when it comes to supplements, which are generally recommended for daily use. However, their sufficient association with cargoes and industrial‐scale production have remained considerable challenges. This study focuses on the development of lipid‐based nanocarriers for CoQ10 by an industrial feasible process that prevents the use of any surfactants or organic solvents.

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“…The mixture was stored at room temperature until the next usage. The compositions of difference PBFs have been presented in Table 1 [10].…”

Section: Preparation Of Pbfmentioning

confidence: 99%

Design and evaluation of a novel nanodrug delivery system for reducing the side effects of clomiphene citrate on endometrium

et al. 2020

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Background Stimulation of ovulation with clomiphene citrate can cause side effects on endometrial receptivity. Formulation with nano-size may be an alternative therapy for women with ovulatory disorders. In this study, we investigated sustained-release clomiphene citrate by using Phosal-based formulation (PBF) and evaluate its decreased side effect on the endometrial receptivity. Methods In the in-vitro study, CC loaded PBF was analyzed using Zetasizer, Fourier-transform infrared spectroscopy (FTIR), and Transmission electron microscopy (TEM). In the in-vivo study, 24 female mice were randomly divided into three groups: CC (5 mg/kg), CC/PBF (5 mg/kg) and SS (1 ml) daily administered and injected with 5 IU HCG and mated after two days. At day 4.5, pregnant mice were euthanized and endometrial tissue was extracted for quantitative polymerase chain reaction (Q-PCR) analysis. ResultsThe optimized PBF contained Phosal 50PG/glycerol in a 2:8 ratios (w/w) and the particle size of optimum formulation was 67 ± 0.30551 nm and the release of CC from CC-containing PBF was slightly faster in the first 24 h; wherein, 29% of CC was released, and 76% of CC was released up to 120 h. The mRNA levels of leukemia inhibitory factor (LIF), leukemia inhibitory factor receptor alpha (LIFR), HOXA10, Heparin-binding epidermal growth factor (HB-EGF), and epidermal growth factor (EGF) were significantly upregulated and MUC1 and PGR mRNA levels were significantly downregulated in the CC-containing PBFtreated animals compared with only CC group (P < 0.05). Conclusion Sustained release formulation of clomiphene citrate increased its targeting efficiency and improved the impact of the CC on implantation.

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Improved Oral Bioavalability of Mebudipine Upon Administration in PhytoSolve and Phosal-Based Formulation (PBF)

Cited by 10 publications

References 16 publications

Non‐Aqueous Phospholipid Concentrates for Increasing the Bioavailability of Poorly Soluble Compounds

Non‐Aqueous Phospholipid Concentrates for Increasing the Bioavailability of Poorly Soluble Compounds

Green Formulation of Triglyceride/Phospholipid‐Based Nanocarriers as a Novel Vehicle for Oral Coenzyme Q10 Delivery

Design and evaluation of a novel nanodrug delivery system for reducing the side effects of clomiphene citrate on endometrium

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