Proliposomes of exemestane for improved oral delivery: Formulation and in vitro evaluation using PAMPA, Caco-2 and rat intestine

Hiremath, Praveen; Soppimath, Kumaresh S.; Betageri, Guru V.

doi:10.1016/j.ijpharm.2009.07.008

Cited by 98 publications

(42 citation statements)

References 31 publications

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“…Different formulation strategies have been employed to overcome the aforementioned biopharmaceutical challenges associated with exemestane such as pro-liposomes [4], polycaprolactone nanoparticles [5], poly (D, L-lactide-co-glycolide)/montmorillonite nanoparticles [6], polymeric nanoparticles [7] and self-emulsifying drug delivery system [3]. However, there are missing studies for lipid nanoparticles.…”

Section: Fig 1: Structure Of Exemestane [3]mentioning

confidence: 99%

Study on Cause–effect Relations and Optimization of Exemestane-Loaded Nanostructured Lipid Carriers

Thang

Hanh

Duong

2017

Int J Pharm Pharm Sci

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Objective: Exemestane is an anti-breast cancer drug, possesses low water solubility and low permeability. This work aimed at the cause-effect relations and optimization of exemestane-loaded nanostructured lipid carriers (EXE-NLCs) for oral delivery.Methods: Excipient screening was based on exemestane solubilities and the emulsification efficiency of surfactants. A D-optimal design based on three independent variables was applied to evaluate the cause-effect relations and optimise EXE-NLCs formulation. The particle size (PS), polydispersity index (PDI), entrapment efficiency (EE) and drug loading (DL) were investigated with respect to three independent variables including liquid lipid to total lipid ratio (X1), surfactant concentration (X2), total lipid concentration (X3).Results: EXE-NLCs were prepared by a hot sonication method employing Labrafac CC and Compritol 888ATO as liquid and solid lipids, respectively, and Cremophor RH40 as a surfactant and Lutrol E-400 as a co-surfactant. All investigated factors: liquid lipid to total lipid ratio, surfactant concentration and total lipid concentration showed significant influences on physicochemical characteristics of EXE-NLCs. The optimal EXE-NLC formulation was composed of liquid lipid to total lipid ratio (X1) of 24 % (w/w), surfactant concentration (X2) of 4 % (w/v) and total lipid concentration (X3) of 4 % (w/v). The PS, PDI, EE and DL of the optimized EXE-NLCs were found to be 41.787 nm; 0.11; 97.605 % and 1.935 %, respectively. The optimized formulation was experimentally examined which demonstrated a good agreement between experimental and predicted values. Conclusion:The cause-effect relations and optimization of EXE-NLCs were investigated and reported for the first time. EXE-NLCs formulation was successfully optimized using D-optimal design and merits further study.

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Section: Fig 1: Structure Of Exemestane [3]mentioning

confidence: 99%

Study on Cause–effect Relations and Optimization of Exemestane-Loaded Nanostructured Lipid Carriers

Thang

Hanh

Duong

2017

Int J Pharm Pharm Sci

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“…Prepared by solvent evaporation method, solid PL formulation containing exemestane, DSPC, and cholesterol at different drug-to-lipid ratios were formulated by (Hiremath et al, 2009). The formulation increased the dissolution of exemestane in PBS pH 7.4 from 9% to about 40% at the end of 60 min.…”

Section: Accepted Manuscriptmentioning

confidence: 99%

Phospholipid-based solid drug formulations for oral bioavailability enhancement: A meta-analysis

Fong

Brandl

Bauer‐Brandl

2015

European Journal of Pharmaceutical Sciences

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“…However, drugs administered by oral route may often result in suboptimal therapeutic response because of the drug's poor solubility, inadequate permeation, and extensive first-pass effect. Proliposomes are reported as drug delivery carriers for enhancing the oral bioavailability of drugs with poor bioavailability (1)(2)(3)(4)(5)(6)(7). Proliposomes are dry, free flowing powders that can form multilamellar vesicles upon hydration.…”

Section: Introductionmentioning

confidence: 99%

Design, Characterization, and In Vivo Pharmacokinetics of Tacrolimus Proliposomes

et al. 2015

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Abstract. The objective of this study was to develop proliposomal formulation for a poorly bioavailable drug, tacrolimus. Proliposomes were prepared by thin film hydration method using different lipids such as hydrogenated soy phosphatidylcholine (HEPC), soy phosphatidylcholine (SPC), distearyl phosphatidylcholine (DSPC), dimyristoylphosphatidylcholine (DMPC), and dimyristoylphosphatidylglycerol sodium (DMPG) and cholesterol in various ratios. Proliposomes were evaluated for particle size, zeta potential, in vitro drug release, in vitro permeability, and in vivo pharmacokinetics. In vitro drug release was carried out in purified water using USP type II dissolution apparatus. In vitro drug permeation was studied using parallel artificial membrane permeation assay (PAMPA) and everted rat intestinal perfusion techniques. In vivo pharmacokinetic studies were conducted in male Sprague-Dawley (SD) rats. Among the different formulations, proliposomes with drug/DSPC/cholesterol in the ratio of 1:2:0.5 demonstrated the desired particle size and zeta potential. Enhanced drug release was observed with proliposomes compared to pure tacrolimus in purified water after 1 h. Tacrolimus permeability across PAMPA and everted rat intestinal perfusion models was significantly higher with proliposomes. The optimized formulation of proliposomes indicated a significant improvement in the rate and absorption of tacrolimus. Following a single oral administration, a relative bioavailability of 193.33% was achieved compared to pure tacrolimus suspension.

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Proliposomes of exemestane for improved oral delivery: Formulation and in vitro evaluation using PAMPA, Caco-2 and rat intestine

Cited by 98 publications

References 31 publications

Study on Cause–effect Relations and Optimization of Exemestane-Loaded Nanostructured Lipid Carriers

Study on Cause–effect Relations and Optimization of Exemestane-Loaded Nanostructured Lipid Carriers

Phospholipid-based solid drug formulations for oral bioavailability enhancement: A meta-analysis

Design, Characterization, and In Vivo Pharmacokinetics of Tacrolimus Proliposomes

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