Elastic Liposomes Mediated Transdermal Deliveryof an Anti-Hypertensive Agent: Propranolol Hydrochloride

Mishra, Dinesh Kumar; Garg, Minakshi; Dubey, Vaibhav; Jain, Subheet Kumar; Jain, Nitin

doi:10.1002/jps.20737

Cited by 100 publications

(57 citation statements)

References 22 publications

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“…RTV13, with a high concentration of PC90G and a medium concentration of SDC, showed maximum flux (ie, 6.5±1.1 µg/cm /hour, respectively; the ER values shown by transfersomal formulation, compared against conventional liposomes and the ethanolic PBS solution, were 6.50 and 9.25, respectively. This enhancement ratio of transdermal flux in the transfersomal system is comparable to a previous finding of Mishra et al 20 A possible explanation for the better performance of the transfersome formulation, compared with conventional liposomes, may be the difference in their flexibility. Being more flexible in their nature, the transfersome vesicles can squeeze themselves through pores much smaller than their own diameters during permeation through the SC.…”

Section: Effect Of Independent Factors On Vesicle Size (Y 2 )supporting

confidence: 87%

“…The amount of phospholipid (A), surfactant (B), and sonication time (C) were selected as independent variables, considering their overall effects on the formulation's stability and transdermal flux, as reported by many researchers. [19][20][21] Accordingly, entrapment efficiency (EE) (Y 1 ), vesicle size (Y 2 ), and transdermal flux (Y 3 ) were selected as dependent variables for the optimization process.…”

Section: Optimization Of Transfersomes Formulationmentioning

confidence: 99%

“…17,18,20,24 However, the ratio of phospholipid and surfactant used in this study was optimized, based on the initial experiments and their observations (data not shown). PC90G concentrations less than 100 mg produced transfersomes with poor values of transdermal flux, whereas PC90G concentrations greater than 300 mg resulted in larger size vesicles, due to aggregation.…”

Section: Working Ranges Of the Independent Variablesmentioning

confidence: 99%

“…PC90G concentrations less than 100 mg produced transfersomes with poor values of transdermal flux, whereas PC90G concentrations greater than 300 mg resulted in larger size vesicles, due to aggregation. 20 In the case of the surfactant, it was observed that too low or too high a concentration of SDC was unsuitable for proper vesicle formation. 19 In both cases, less than 15 mg or more than 55 mg of surfactant resulted in very low entrapment efficiency, as well as low transdermal flux.…”

Section: Working Ranges Of the Independent Variablesmentioning

confidence: 99%

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Experimental design and optimization of raloxifene hydrochloride loaded nanotransfersomes for transdermal application

Mahmood¹,

Taher²,

Mandal³

2014

IJN

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Raloxifene hydrochloride, a highly effective drug for the treatment of invasive breast cancer and osteoporosis in post-menopausal women, shows poor oral bioavailability of 2%. The aim of this study was to develop, statistically optimize, and characterize raloxifene hydrochloride-loaded transfersomes for transdermal delivery, in order to overcome the poor bioavailability issue with the drug. A response surface methodology experimental design was applied for the optimization of transfersomes, using Box-Behnken experimental design. Phospholipon ® 90G, sodium deoxycholate, and sonication time, each at three levels, were selected as independent variables, while entrapment efficiency, vesicle size, and transdermal flux were identified as dependent variables. The formulation was characterized by surface morphology and shape, particle size, and zeta potential. Ex vivo transdermal flux was determined using a Hanson diffusion cell assembly, with rat skin as a barrier medium. Transfersomes from the optimized formulation were found to have spherical, unilamellar structures, with a homogeneous distribution and low polydispersity index (0.08). They had a particle size of 134±9 nM, with an entrapment efficiency of 91.00%±4.90%, and transdermal flux of 6.5±1.1 μg/cm 2 /hour. Raloxifene hydrochloride-loaded transfersomes proved significantly superior in terms of amount of drug permeated and deposited in the skin, with enhancement ratios of 6.25±1.50 and 9.25±2.40, respectively, when compared with drug-loaded conventional liposomes, and an ethanolic phosphate buffer saline. Differential scanning calorimetry study revealed a greater change in skin structure, compared with a control sample, during the ex vivo drug diffusion study. Further, confocal laser scanning microscopy proved an enhanced permeation of coumarin-6-loaded transfersomes, to a depth of approximately160 μM, as compared with rigid liposomes. These ex vivo findings proved that a raloxifene hydrochloride-loaded transfersome formulation could be a superior alternative to oral delivery of the drug.

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Section: Effect Of Independent Factors On Vesicle Size (Y 2 )supporting

confidence: 87%

Section: Optimization Of Transfersomes Formulationmentioning

confidence: 99%

Section: Working Ranges Of the Independent Variablesmentioning

confidence: 99%

Section: Working Ranges Of the Independent Variablesmentioning

confidence: 99%

See 2 more Smart Citations

Experimental design and optimization of raloxifene hydrochloride loaded nanotransfersomes for transdermal application

Mahmood¹,

Taher²,

Mandal³

2014

IJN

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“…However, the effectiveness of a vesicular system is strongly dependent on its physicochemical characteristics, in particular its thermodynamic state. Deformable vesicles like elastic liposomes have been found to be more effective in enhancing drug transport as compared to rigid vesicles like conventional liposomes for number of drug molecules like dexamethasone (10), diclofenac (11), zidovudine (12), lamivudine (13), propranolol (14), and rizatriptan (15). It was found that high elasticity of these vesicles could facilitate drug transport across the skin as compared to vesicles with rigid membranes.…”

Section: Introductionmentioning

confidence: 99%

Elastic Liposomal Formulation for Sustained Delivery of Colchicine: In Vitro Characterization and In Vivo Evaluation of Anti-gout Activity

Singh

Utreja

Tiwary

et al. 2009

AAPS J

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Abstract. Colchicine, an alkaloid found in extracts of the plants Colchicum autumnale and Gloriosa superb, is effective in the treatment of acute gout and dermatological conditions like leuko-cytoclastic vasculitis, psoriasis, and Sweet's syndrome. Oral administration of colchicine is associated with gastrointestinal side effects and its accumulation in the body leads to bone marrow suppression. In the present study, an attempt has been made for development and in vitro and in vivo evaluation of elastic liposomal formulation for topical delivery of colchicine. The in vitro skin permeation study across rat skin found transdermal flux for different elastic liposomal formulations to range between 32.8±1.2 and 44.4± 1.9 μg h −1 cm −2 , which was approximately seven to 11 times higher than obtained using drug solution (4.3± 0.6 μg h −1 cm −2 ). The results of skin deposition study showed that elastic liposomal formulation provide 12.5-fold higher skin deposition as compared to drug solution of colchicine. Confocal laser scanning microscopy also revealed better accumulation and deeper penetration (up to 200 μm) of elastic liposomes than drug solution (up to 12 μm). The biological evaluation of various vesicular formulations and drug solution was carried out using monosodium urate-induced air pouch model. The results of anti-gout activity in rats showed better and sustained biological effects in 24 h measured in terms of exudate volume (63.1± 5.7% and 9.6±0.5% reduction with elastic liposomes and drug solution, respectively), reduction in leukocyte count (74.2±6.0% and 4.1±0.3% reduction with elastic liposomes and drug solution, respectively), decrease in inflammatory cells accumulation, and collagen deposition with elastic liposomal formulation than drug solution. Hence, the present study reveals that elastic liposomal formulation of colchicine possesses greater potential to enhance skin accumulation, prolong drug release, and improve the site-specificity of colchicine.

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Methodologies Used for the Characterization of Nano‐ and Microcapsules

Nguyen

Aripin

Chen

et al. 2014

Nano‐ and Microencapsulation for Foods

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Elastic Liposomes Mediated Transdermal Deliveryof an Anti-Hypertensive Agent: Propranolol Hydrochloride

Cited by 100 publications

References 22 publications

Experimental design and optimization of raloxifene hydrochloride loaded nanotransfersomes for transdermal application

Experimental design and optimization of raloxifene hydrochloride loaded nanotransfersomes for transdermal application

Elastic Liposomal Formulation for Sustained Delivery of Colchicine: In Vitro Characterization and In Vivo Evaluation of Anti-gout Activity

Methodologies Used for the Characterization of Nano‐ and Microcapsules

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