Preparation, Characterization and In-Vitro Release Study of Flurbiprofen Loaded Stealth Liposomes

Begum, M. Yasmin; Abbulu, K; Sudhakar, M.

doi:10.7598/cst2012.108

Cited by 17 publications

(11 citation statements)

References 18 publications

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“…In both cases, the DOPC:DSPG mixture exhibited the higher value. These observations, are in line with the report that longer alkyl chain lipids enhance the binding of the drug with the lipid bilayer, resulting in slower or sustained drug release [57].…”

Section: Particle Size Distributionsupporting

confidence: 81%

Comparative Study of PEGylated and Conventional Liposomes as Carriers for Shikonin

Tsermentseli

Kontogiannopoulos

Papageorgiou

et al. 2018

Fluids

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Abstract:Liposomes are considered to be one of the most successful drug delivery systems.They apply nanotechnology to potentiate the therapeutic efficacy and reduce the toxicity of conventional medicines. Shikonin and alkannin, a pair of chiral natural naphthoquinone compounds, derived from Alkanna and Lithospermum species, are widely used due to their various pharmacological activities, mainly wound healing, antioxidant, anti-inflammatory and their recently established antitumor activity. The purpose of this study was to prepare conventional and PEGylated shikonin-loaded liposomal formulations and measure the effects of different lipids and polyethylene glycol (PEG) on parameters related to particle size distribution, the polydispersity index, the zeta potential, drug-loading efficiency and the stability of the prepared formulations. Three types of lipids were assessed (1,2-Dioleoyl-sn-glycero-3-phosphocholine (DOPC), 1,2-Distearoyl-sn-glycero-3-phosphocholine (DSPC) and 1,2-distearoyl-sn-glycero-3-phospho-rac-(1-glycerol) (DSPG)), separately and in mixtures, forming anionic liposomes with good physicochemical characteristics, high entrapment efficiencies (varying from 56.5 to 89.4%), satisfactory in vitro release profiles and good physical stability. The addition of the negatively charged DSPG lipids to DOPC, led to an increment in the drug's incorporation efficiency and reduced the particle size distribution. Furthermore, the shikonin-loaded PEGylated sample with DOPC/DSPG, demonstrated the most satisfactory characteristics. These findings are considered promising and could be used for further design and improvement of such formulations.

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Section: Particle Size Distributionsupporting

confidence: 81%

Comparative Study of PEGylated and Conventional Liposomes as Carriers for Shikonin

Tsermentseli

Kontogiannopoulos

Papageorgiou

et al. 2018

Fluids

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“…The frequency of absorption due to the carbonyl group depends mainly on the force constant which in turn depends upon inductive effect, conjugative effect, field effect, stearic effects. The shifts seen due to the above mentioned interaction may however support the formation of favorable vesicle shape, structure with good stability and sustained drug release [37].…”

Section: Fourier-transform Infrared Spectroscopy (Ft-ir)mentioning

confidence: 99%

In-vitro and In-vivo Evaluation of Niosomal Gel Containing Aceclofenac for Sustained Drug Delivery

Fathalla¹

2014

Int J Pharm Sci Res

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Background: Niosomes are non-ionic stable vesicular system, which can accommodate both hydrophobic and hydrophilic drugs. The aim of the present study was to prepare and characterize niosomal gel formulations for sustained delivery of aceclofenac. Aceclofenac is the most widely used anti-inflammatory agent in the treatment of rheumatoid arthritis. It has narrow therapeutic index and short biological half-life. Methods: Aceclofenac loaded niosomes were prepared using reverse phase evaporation technique. The effects of concentration of non-ionic surfactant, cholesterol and concentration of drug on the encapsulation efficiency were studied. The formulations were characterized using different techniques, such as differential scanning calorimetry (DSC), fourier-transform infrared spectroscopy (FTIR), optical microscope and transmission electron microscope (TEM). Selected formulations of niosomes were incorporated into carbopol 934 (1%w/w), sodium alginate (7%w/w), sodium carboxy methyl cellulose (3% w/w), pluronic F127 (20%w/w) and HPMC (3% w/w) gels. The niosomal gel formulations were evaluated for in-vitro drug release and skin permeation. Optimum niosomal gel formulation was evaluated in-vivo using carrageenen-induced rat paw edema test and compared to gel containing the drug alone. Results: TEM analysis confirmed that niosomal samples were spherical in shape and have a definite internal aqueous space. Niosomes of span60 showed higher percent drug entrapment and larger particle size. In-vitro drug release and skin permeation of different gel preparations showed sustained release and enhanced permeation compared to gel formulations containing free drug. Among the niosomal gel formulations, HPMC gel showed the highest release rate of the drug. The in-vivo anti-inflammatory activity of the selected niosomal gel formulation was significantly higher and more sustained than the corresponding non-niosomal gel formulation containing free drug. Conclusion:These results suggest that the niosome-containing gels are promising formulations for sustained local delivery of aceclofenac.

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“…The drug‐excipient interaction was studied before developing the formulation by using FTIR‐spectroscopy. The shifts observed in the IR spectrum of CXB‐loaded liposomes may be due to the formation of hydrogen bonds, Van der Walls forces or the dipole moment of the polar functional groups of CXB, and the excipients that may support favorable vesicle shape and structure with good stability and sustained drug release [Begum et al., ]. The absence of the melting endotherm of CXB in the DSC thermogram suggested a significant interaction of the drug, with the bilayer leading to increased drug entrapment and sustained release.…”

Section: Discussionmentioning

confidence: 99%

Liposomal Gels for Site‐Specific, Sustained Delivery of Celecoxib: In Vitro and In Vivo Evaluation

Fetih

Fathalla

El-Badry

2014

Drug Development Research

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The objective of this work was to evaluate liposome-containing gel formulations for the sustained, site-specific delivery of celecoxib (CXB). Liposomes composed of phosphadtidylcholine (and various amounts of cholesterol (Ch) were prepared using thin film hydration and characterized for encapsulation efficiency, vesicle size, and drug-excipient interaction using differential scanning calorimetry and Fourier-transform infrared spectroscopy. The selected liposome formulation was incorporated in different gel formulations: the Ch ratio affected the encapsulation efficiency of the drug, by increasing Ch ratio up until 1:1 the encapsulation efficiency increased. Further increasing the Ch ratio resulted in decreasing encapsulation efficiency. In vitro drug release and skin permeation studies showed sustained release and enhanced permeation compared with gel formulations containing free drug. In the rat paw edema test, the anti-inflammatory activity of the selected liposomal gel formulation was higher and more sustained compared with that of the nonliposomal gel formulation containing free drug. These results suggest that the liposome-containing gels are promising formulations for sustained, site-specific delivery of CXB.

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Preparation, Characterization and In-Vitro Release Study of Flurbiprofen Loaded Stealth Liposomes

Cited by 17 publications

References 18 publications

Comparative Study of PEGylated and Conventional Liposomes as Carriers for Shikonin

Comparative Study of PEGylated and Conventional Liposomes as Carriers for Shikonin

In-vitro and In-vivo Evaluation of Niosomal Gel Containing Aceclofenac for Sustained Drug Delivery

Liposomal Gels for Site‐Specific, Sustained Delivery of Celecoxib: In Vitro and In Vivo Evaluation

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