Development and optimization of ketoconazole loaded nano-transfersomal gel for vaginal delivery using Box-Behnken design: In vitro , ex vivo characterization and antimicrobial evaluation

Singh, Shalu; Verma, Devina; Mirza, Mohd. Aamir; Das, Ayan Kumar; Dudeja, Mridu; Anwer, Md. Khalid; Sultana, Yasmin; Talegaonkar, Sushama; Iqbal, Zeenat

doi:10.1016/j.jddst.2017.03.007

Cited by 47 publications

(17 citation statements)

References 13 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The measurements were accomplished at a constant shear speed (40 rpm) and varying shear speeds (2–120 rpm) with a 64-number spindle. The apparent viscosity of the gel formulations at each speed was recorded and the flow pattern was established from the rheogram (Singh et al., 2017 ).…”

Section: Methodsmentioning

confidence: 99%

Sodium stibogluconate loaded nano-deformable liposomes for topical treatment of leishmaniasis: macrophage as a target cell

2018

View full text Add to dashboard Cite

Topical drug delivery against cutaneous leishmaniasis (CL) signifies an effective alternate for improving the availability and reducing the toxicity associated with the parenteral administration of conventional sodium stibogluconate (SSG) injection. The basic aim of the study was to develop nano-deformable liposomes (NDLs) for the dermal delivery of SSG against CL. NDLs were formulated by a modified thin film hydration method and optimized via Box–Behnken statistical design. The physicochemical properties of SSG-NDLs were established in terms of vesicle size (195.1 nm), polydispersity index (0.158), zeta potential (−32.8 mV), and entrapment efficiency (35.26%). Moreover, deformability index, in vitro release, and macrophage uptake studies were also accomplished. SSG-NDLs were entrapped within Carbopol gel network for the ease of skin application. The ex vivo skin permeation study revealed that SSG-NDLs gel provided 10-fold higher skin retention towards the deeper skin layers, attained without use of classical permeation enhancers. Moreover, in vivo skin irritation and histopathological studies verified safety of the topically applied formulation. Interestingly, the cytotoxic potential of SSG-NDLs (1.3 mg/ml) was higher than plain SSG (1.65 mg/ml). The anti-leishmanial activity on intramacrophage amastigote model of Leishmania tropica showed that IC50 value of the SSG-NDLs was ∼ fourfold lower than the plain drug solution with marked increase in the selectivity index. The in vivo results displayed higher anti-leishmanial activity by efficiently healing lesion and successfully reducing parasite burden. Concisely, the outcomes indicated that the targeted delivery of SSG could be accomplished by using topically applied NDLs for the effective treatment of CL.

show abstract

Section: Methodsmentioning

confidence: 99%

Sodium stibogluconate loaded nano-deformable liposomes for topical treatment of leishmaniasis: macrophage as a target cell

2018

View full text Add to dashboard Cite

show abstract

“…Celecoxib transfersomal gel for the rheumatoid arthritis treatment showed the release of 75% of the entrapped drug within 6 h, which is more than a 30% increment relative to the commercial gel [ 92 ]. Ketoconazole-loaded transfersomal gel showed an initial burst of the drug release of 40.67%, which was higher than that of ketoconazole suspension (27.35%) after 6 h [ 93 ]. The in vitro release profile of lidocaine from the transfersomal vesicles showed more than 80% of the drug released after 6 h [ 94 ].…”

Section: Characterization Of the Transfersomesmentioning

confidence: 99%

“…The receptor compartments of the Franz diffusion cells are filled with phosphate buffer saline solution, which is stirred by a magnetic bar. As the receptor fluid is used to mimic blood circulation beneath the skin, the temperature of the receptor fluid should be kept at 37 ± 0.5 °C [ 40 , 93 ]. An appropriate amount of the testing formulation is added into each donor compartment as it is placed on the membrane, and the top of the diffusion cell is opened to mimic nonoccluded conditions.…”

Section: Characterization Of the Transfersomesmentioning

confidence: 99%

Transfersomes: A Promising Nanoencapsulation Technique for Transdermal Drug Delivery

2020

View full text Add to dashboard Cite

Transdermal delivery systems have gained much interest in recent years owing to their advantages compared to conventional oral and parenteral delivery systems. They are noninvasive and self-administered delivery systems that can improve patient compliance and provide a controlled release of the therapeutic agents. The greatest challenge of transdermal delivery systems is the barrier function of the skin’s outermost layer. Molecules with molecular weights greater than 500 Da and ionized compounds generally do not pass through the skin. Therefore, only a limited number of drugs are capable of being administered by this route. Encapsulating the drugs in transfersomes are one of the potential approaches to overcome this problem. They have a bilayered structure that facilitates the encapsulation of lipophilic and hydrophilic, as well as amphiphilic, drug with higher permeation efficiencies compared to conventional liposomes. Transfersomes are elastic in nature, which can deform and squeeze themselves as an intact vesicle through narrow pores that are significantly smaller than its size. This review aims to describe the concept of transfersomes, the mechanism of action, different methods of preparation and characterization and factors affecting the properties of transfersomes, along with their recent applications in the transdermal administration of drugs.

show abstract

“…The gel was prepared by dispersing carbopol (1%w/v) in a beaker with continuous stirring at 200 rpm for 2 hours, after complete dispersion, it was kept for swelling overnight then sonicated for 30 minutes. To the prepared blank gel, optimized IBU loaded TFs (TFs2) was incorporated with continuous stirring with glass rod until homogeneous mixture formed, and finally triethanolamine was added as neutralizing agent [21].…”

Section: Preparation Of Ibu Loaded Transferosomal Gelmentioning

confidence: 99%

Formulation, Development and Evaluation of Ibuprofen Loaded Nano-transferosomal Gel for the Treatment of Psoriasis

Abdallah

Lila

Anwer

et al. 2019

JPRI

Self Cite

View full text Add to dashboard Cite

The present work was aimed to develop a transferosomal gel of ibuprofen (IBU) for the amelioration of psoriasis like inflammation. Three formulation of IBU loaded transferosomes (TFs1-TFs3) were prepared using different proportions of lipid (phospholipon 90H) and surfactant (tween 80) and further evaluated for vesicle size, zeta potential (ZP), entrapment efficiency and in vitro drug release. The IBU loaded transferosomes (TFs2) was optimized with vesicle size (217±8.4 nm), PDI (0.102), ZP (-31.5±4.3 mV), entrapment efficiency (88.4±6.9%) and drug loading (44.2±2.9%). Further, the optimized IBU loaded transferosomes (TFs2) was incorporated into 1% carbopol 934 gel base and characterized for homogeneity, extrudability, viscosity and drug content. The in vivo pharmacodynamic study of gel exhibited reduction in psoriasis like inflammation in mice. The ibuprofen loaded transferosomal gel was successfully developed and has shown the potential to be a new therapy against psoriasis like inflammation.

show abstract

Development and optimization of ketoconazole loaded nano-transfersomal gel for vaginal delivery using Box-Behnken design: In vitro , ex vivo characterization and antimicrobial evaluation

Cited by 47 publications

References 13 publications

Sodium stibogluconate loaded nano-deformable liposomes for topical treatment of leishmaniasis: macrophage as a target cell

Sodium stibogluconate loaded nano-deformable liposomes for topical treatment of leishmaniasis: macrophage as a target cell

Transfersomes: A Promising Nanoencapsulation Technique for Transdermal Drug Delivery

Formulation, Development and Evaluation of Ibuprofen Loaded Nano-transferosomal Gel for the Treatment of Psoriasis

Contact Info

Product

Resources

About