Increasing bioavailability of silymarin using a buccal liposomal delivery system: Preparation and experimental design investigation

El-Samaligy, Mohamed S.; Afifi, Nagia N.; Mahmoud, E. A.

doi:10.1016/j.ijpharm.2005.11.006

Cited by 182 publications

(98 citation statements)

References 33 publications

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“…Dialysis method was applied using a Spectra/Pore® dialysis membrane (12,000-14,000 molecular weight cutoff). This membrane assures the permeation of the drug and at same time retains liposomal forms (27).…”

Section: Determination Of Ciprofloxacin Entrapment Efficiency In Lipomentioning

confidence: 99%

“…Activity of liposomes as a carrier for drugs depends upon various factors such as charge, rigidity, composition of the liposomal membrane, encapsulation efficiency and release rate (21)(22)(23)(24). Liposomes can be formulated from a variety of lipid and lipid mixtures with different composition (25), they can be modified in particle size, structure, and surface charge to obtain desirable physicochemical properties to suit particular needs (26,27).…”

Section: Introductionmentioning

confidence: 99%

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Ciprofloxacin as Ocular Liposomal Hydrogel

Hosny

2010

AAPS PharmSciTech

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Abstract. The purpose of this study was to prepare and characterize an ocular effective prolonged-release liposomal hydrogel formulation containing ciprofloxacin. Reverse-phase evaporation was used for preparation of liposomes consisting of soybean phosphatidylcholine (PC) and cholesterol (CH). The effect of PC/CH molar ratio on the percentage drug encapsulation was investigated. The effect of additives such as stearylamine (SA) or dicetyl phosphate (DP) as positive and negative charge inducers, respectively, were studied. Morphology, mean size, encapsulation efficiency, and in vitro release of ciprofloxacin from liposomes were evaluated. For hydrogel preparation, Carbopol 940 was applied. In vitro transcorneal permeation through excised albino rabbit cornea was also determined. Optimal encapsulation efficiency of 73.04±3.06% was obtained from liposomes formulated with PC/CH at molar ratio of 5:3 and by increasing CH content above this limit, the encapsulation decreased. Positively charged liposomes showed superior entrapment efficiency (82.01±0.52) over the negatively charged and the neutral liposomes. Hydrogel containing liposomes with lipid content PC, CH, and SA in molar ratio 5:3:1, respectively, showed the best release and transcorneal permeation with the percentage permeation of 30.6%. These results suggest that the degree of encapsulation of ciprofloxacin into liposomes and prolonged in vitro release depend on composition of the vesicles. In addition, the polymer hydrogel used in preparation ensure steady and prolonged transcorneal permeation. In conclusion, ciprofloxacin liposomal hydrogel is a suitable delivery system for improving the ocular bioavailability of ciprofloxacin.

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Section: Determination Of Ciprofloxacin Entrapment Efficiency In Lipomentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Ciprofloxacin as Ocular Liposomal Hydrogel

Hosny

2010

AAPS PharmSciTech

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“…Recently, the cancer preventive activity of silybin has been reported in many literatures (Ramasamy & Agarwal, 2008;Zhang et al, 2013b;Liang et al, 2014). Despite the promising therapeutic potential, the application of silybin is limited by low oral bioavailability, owing to its low solubility in water, poor absorption from gastrointestinal tract and degradation in gastrointestinal fluids (El-Samaligy et al, 2006;Wang et al, 2014). In order to overcome these biopharmaceutical challenges, researches have focused on the development of new oral or parenteral drug delivery systems (DDS) of silybin to improve the solubility and bioavailability Cao et al, 2013;Angelico et al, 2014).…”

Section: Introductionmentioning

confidence: 99%

Liver-targeting self-assembled hyaluronic acid-glycyrrhetinic acid micelles enhance hepato-protective effect of silybin after oral administration

Han

Wang

et al. 2015

Drug Delivery

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Muxin Gong (2016) Liver-targeting self-assembled hyaluronic acidglycyrrhetinic acid micelles enhance hepato-protective effect of silybin after oral administration, Drug Delivery, 23:5, 1818-1829, DOI: 10.3109/10717544.2015 AbstractIn order to enhance oral bioavailability and liver targeting delivery of silybin, two amphiphilic hyaluronic acid derivatives, hyaluronic acid-deoxycholic acid (HA-adh-DOCA) and hyaluronic acid-glycyrrhetinic acid (HA-adh-GA) conjugates, were designed and synthesized. Silybin was successfully loaded in HA-adh-DOCA and HA-adh-GA micelles with high drug-loading capacities (20.3% ± 0.5% and 20.6% ± 0.6%, respectively). The silybin-loaded micelles were spherical in shape with the average size around 130 nm. In vitro release study showed that two silybin-loaded micelles displayed similar steady continued-release pattern in simulated gastrointestinal fluids and PBS. Single-pass intestinal perfusion studies indicated that silybinloaded micelles were absorbed in the whole intestine and transported via a passive diffusion mechanism. Compared with suspension formulation, silybin-loaded HA-adh-DOCA and HA-adh-GA micelles achieved significantly higher AUC and C max level. Moreover, liver targeting drug delivery of micelles was confirmed by in vivo imaging analysis. In comparison between the two micellar formulations, HA-adh-GA micelles possessed higher targeting capacity than HA-adh-DOCA micelles, owing to the active hepatic targeting properties of glycyrrhetinic acid. In the treatment of acute liver injury induced by CCl 4 , silybin-loaded HA-adh-GA micelles displayed better effects over suspension control and silybin-loaded HA-adh-DOCA micelles. Overall, pharmaceutical and pharmacological indicators suggested that the HA-adh-GA conjugates can be successfully utilized for liver targeting of orally administered therapeutics.

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“…Silymarin was selected as a model hydrophobic drug for the present study. Low aqueous solubility and poor bioavailability of silymarin (18,19) make it a suitable candidate for design into nanoparticulate drug delivery systems.…”

Section: Introductionmentioning

confidence: 99%

Nanoparticles of Polyethylene Sebacate: A New Biodegradable Polymer

Guhagarkar

Malshe²,

Devarajan

2009

AAPS PharmSciTech

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Abstract. The present study demonstrates feasibility of preparation of nanoparticles using a novel polymer, polyethylene sebacate (PES), and its application in the design of drug-loaded nanocarriers. Silymarin was selected as a model hydrophobic drug for the present study. Two methods of preparation, viz., nanoprecipitation and emulsion solvent diffusion, were evaluated for preparation of nanoparticles. Effect of surfactants polyvinyl alcohol (PVA), lutrol F 68, and Tween 80 on the preparation of blank and silymarin-loaded PES nanoparticles was evaluated. Nanoprecipitation resulted in the formation of nanoparticles with all the surfactants (<450 nm). Increase in surfactant concentration resulted in decrease in entrapment efficiency and particle size except with PVA. The type and concentration of surfactant was critical to achieve low size and adequate drug entrapment. While increase in concentration of PES resulted in larger nanoparticles, inclusion of acetone in the organic phase resulted in particles of smaller size. In case of emulsion solvent diffusion, nanoparticles were obtained only with lutrol F 68 as surfactant and high surfactant concentration. The study revealed nanoprecipitation as a more versatile method for preparation of PES nanoparticles. Scanning electron microscopy studies revealed spherical shape of nanoparticles. Freeze-dried nanoparticles exhibited ease of redispersion, with a marginal increase in size. Differential scanning calorimetry and X-ray diffraction analysis revealed amorphous nature of the drug. The study demonstrates successful design of PES nanoparticles as drug carriers.

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Increasing bioavailability of silymarin using a buccal liposomal delivery system: Preparation and experimental design investigation

Cited by 182 publications

References 33 publications

Ciprofloxacin as Ocular Liposomal Hydrogel

Ciprofloxacin as Ocular Liposomal Hydrogel

Liver-targeting self-assembled hyaluronic acid-glycyrrhetinic acid micelles enhance hepato-protective effect of silybin after oral administration

Nanoparticles of Polyethylene Sebacate: A New Biodegradable Polymer

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