Proliposomes for oral delivery of dehydrosilymarin: preparation and evaluation in vitro and in vivo

Chu, Chang Ying; Tong, Shanshan; Xu, Ying; Wang, Li; Fu, Min; Ge, Yanru; Yu, Jiangnan; Xu, Ximing

doi:10.1038/aps.2011.25

Cited by 90 publications

(41 citation statements)

References 30 publications

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“…The sample tubes were centrifuged at 2500 rpm for 20 min at room temperature. The encapsulated tacrolimus liposomes remain on the surface of the filter membrane, and free drug was collected into the bottom tube of the filter (38). The separated phase was transferred to a 10-mL flask, diluted to volume with ethanol, and analyzed using the HPLC method.…”

Section: Encapsulation Efficiencymentioning

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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Section: Encapsulation Efficiencymentioning

confidence: 99%

Design, Characterization, and In Vivo Pharmacokinetics of Tacrolimus Proliposomes

et al. 2015

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“…In vitro-in vivo correlation (IVIVC) refers to the predictive mathematical model describing the relationship between in vitro dissolution and in vivo input rate [21] . Although four categories of IVIVCs have been described in the FDA guidance, a level A correlation model is used to describe the relationship because that is considered most informative and very useful from a regulatory viewpoint.…”

Section: In Vitro-in Vivo Correlationmentioning

confidence: 99%

Oral delivery of capsaicin using MPEG-PCL nanoparticles

et al. 2014

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Aim: To prepare a biodegradable polymeric carrier for oral delivery of a water-insoluble drug capsaicin (CAP) and evaluate its quality. Methods: CAP-loaded methoxy poly (ethylene glycol)-poly(ε-caprolactone) nanoparticles (CAP/NPs) were prepared using a modified emulsification solvent diffusion technique. The quality of CAP/NPs were evaluated using transmission electron microscopy, powder X-ray diffraction, differential scanning calorimetry and Fourier transform infrared techniques. A dialysis method was used to analyze the in vitro release profile of CAP from the CAP/NPs. Adult male rats were orally administered CAP/NPs (35 mg/kg), and the plasma concentrations of CAP were measured with a validated HPLC method. The morphology of rat gastric mucosa was studied with HE staining. Results: CAP/NPs had an average diameter of 82.54±0.51 nm, high drug-loading capacity of 14.0%±0.13% and high stability. CAP/NPs showed a biphasic release profile in vitro: the burst release was less than 25% of the loaded drug within 12 h followed by a more sustained release for 60 h. The pharmacokinetics study showed that the mean maximum plasma concentration was observed 4 h after oral administered of CAP/NPs, and approximately 90 ng/mL of CAP was detected in serum after 36 h. The area under the curve for the CAP/NPs group was approximately 6-fold higher than that for raw CAP suspension. Histological studies showed that CAP/NPs markedly reduced CAP-caused gastric mucosa irritation. Conclusion: CAP/NPs significantly enhance the bioavailability of CAP and markedly reduce gastric mucosa irritation in rats.

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“…Lip-Se were composed of DPPC, DSPG, and Chol and prepared using the thin film evaporation technique by using reported methods with slight variations (41)(42)(43). Lip-Se I, Lip-Se II, Man-Lip-Se I, and Man-Lip-Se II formulations were prepared as described in Fig.…”

Section: Preparation Of Selenium-loaded Nanoliposomesmentioning

confidence: 99%

Freeze-Dried Targeted Mannosylated Selenium-Loaded Nanoliposomes: Development and Evaluation

et al. 2013

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Abstract. The aim of this investigation was to develop and evaluate freeze-dried mannosylated liposomes for the targeted delivery of selenium. Dipalmitoylphosphatidylcholine, distearoylphosphatidylglycerol, and cholesterol were dissolved in a chloroform and methanol mixture and allowed to form a thin film within a rotatory evaporator. This thin film was hydrated with a sodium selenite (5.8 μM) solution to form multilamellar vesicles and homogenized under high pressure to yield unilamellar nanoliposomes. Seloaded nanoliposomes were mannosylated by 0.1%w/v mannosamine (Man-Lip-Se) prior to being lyophilized. Mannosamine concentration was optimized with cellular uptake studies in M receptor expressing cells. Non-lyophilized and lyophilized Man-Lip-Se were characterized for size, zeta potential, and entrapment efficiency. The influence of liposomal composition on the characteristics of Man-Lip-Se were evaluated using acidic and basic medium for 24 h. Thermal analysis and powder X-ray diffraction were used to determine the interaction of components within the Man-Lip-Se. The size, zeta potential and entrapment efficiency of the optimum Man-Lip-Se were observed to be 158±28.9 nm, 33.21±0.89 mV, and 77.27±2.34%, respectively. An in vitro Se release of 70-75% up to 24 h in PBS pH 6.8 and <8% Se release in acidic media (0.1 N HCl) in 1 h was observed. The Man-Lip-Se were found to withstand gastric-like environments and showed sustained release. Stable freeze-dried Man-Lip-Se were successfully formulated with a size of <200 nm, ∼75% entrapment, and achieved controlled release of Se with stability under acidic media, which may be of importance in the targeted delivery of Se to the immune system.

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Proliposomes for oral delivery of dehydrosilymarin: preparation and evaluation in vitro and in vivo

Cited by 90 publications

References 30 publications

Design, Characterization, and In Vivo Pharmacokinetics of Tacrolimus Proliposomes

Design, Characterization, and In Vivo Pharmacokinetics of Tacrolimus Proliposomes

Oral delivery of capsaicin using MPEG-PCL nanoparticles

Freeze-Dried Targeted Mannosylated Selenium-Loaded Nanoliposomes: Development and Evaluation

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