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

Objective: The objective of this study was to develop a novel formulation (Phytosome) of umbelliferone with phospholipid for improved permeability, solubility and hence better pharmacological action.Methods: The phytosomal complex was prepared by using solvent evaporation method and optimised by applying the Box-Behnken design on the basis of complexation rate and partition coefficient. The formation of phytosomes was confirmed by FTIR, DSC, SEM, XRD, HPTLC and NMR by comparing the results of the complex with the drug. The photoprotective potential of complex against UV-exposure was evaluated in rats and compared with the drug by incorporating it in a gel and estimating the antioxidant enzymes in skin namely reduced glutathione, superoxide dismutase, lipid peroxidation and catalase.Results: The crystalline drug was completely converted to amorphous complex. The complex showed a good practical yield, drug content and particle size was in the range. The solubility of the complex was determined by partition coefficient method and was found to be better than the drug. The ex vivo and in-vitro permeation of the complex showed improved permeation for complex than the drug. The in vitro antioxidant activity of complex was evaluated by DPPH and ferrozine antioxidant assay and was better than the drug. The photoprotective action of the complex was found to be better than drug on the basis of the content of antioxidant enzymes estimated in the skin.Conclusion: The phytosomal complex was found to show better solubility in the water phase and oil phase, better permeation, better antioxidant activity and a better photo-protective activity when compared to umbelliferone.

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Development and optimization of sulforaphane-loaded nanostructured lipid carriers by the Box-Behnken design for improved oral efficacy against cancer: in vitro, ex vivo and in vivo assessments

Artificial Cells Nanomedicine and Biotechnology ◽

10.1080/21691401.2017.1408124 ◽

2017 ◽

Vol 46 (sup1) ◽

pp. 15-31 ◽

Cited By ~ 24

Author(s):

Kriti Soni ◽

Md. Rizwanullah ◽

Kanchan Kohli

Keyword(s):

Ex Vivo ◽

Nanostructured Lipid Carriers ◽

Box Behnken Design

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Design and Optimization of Cationic Nanocapsules for Topical Delivery of Tretinoin: Application of the Box-Behnken Design, In Vitro Evaluation, and Ex Vivo Skin Deposition Study

BioMed Research International ◽

10.1155/2021/4603545 ◽

2021 ◽

Vol 2021 ◽

pp. 1-13

Author(s):

Saeed Ebrahimi ◽

Reza Mahjub ◽

Rasool Haddadi ◽

Seyed Yaser Vafaei

Keyword(s):

Particle Size ◽

Ex Vivo ◽

Skin Permeation ◽

Skin Irritation ◽

In Vitro Release ◽

Topical Delivery ◽

Free Drug ◽

Acrylic Polymer ◽

Box Behnken Design

Cationic nanocapsules represent a promising approach for topical delivery purposes. We elaborated on a novel formulation based on the cationic nanocapsules to enhance the pharmacodynamic efficacy, user compliance, and photostability of tretinoin (TTN). To achieve this goal, TTN nanocapsules were prepared by the nanoprecipitation method. In order to statistically optimize formulation variables, a Box-Behnken design, using Design-Expert software, was employed. Three independent variables were evaluated: total weight of the cationic acrylic polymer ( X 1 ), oil volume ( X 2 ), and TTN amount ( X 3 ). The particle size and encapsulation efficiency percent (EE%) were selected as dependent variables. The optimal formulation demonstrated spherical morphology under scanning electron microscopy (SEM), optimum particle size of 116.3 nm, and high EE% of 83.2%. TTN-loaded nanocapsules improved photostability compared to its methanolic solution. The in vitro release study data showed that tretinoin was released in a sustained manner compared to the free drug. The ex vivo skin permeation study demonstrated that greater drug deposition into the epidermal region rather than the deep skin was observed with a gel containing TTN-loaded nanocapsules than that of drug solution, respectively. The skin irritation test revealed that the nanoencapsulation of the drug decreased its irritancy compared to the free drug. These results revealed the promising potential of cationic nanocapsules for topical delivery of tretinoin

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FORMULATION, SYSTEMATIC OPTIMIZATION, IN VITRO, EX VIVO, AND STABILITY ASSESSMENT OF TRANSETHOSOME BASED GEL OF CURCUMIN

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2018.v11s2.28563 ◽

2018 ◽

Vol 11 (14) ◽

pp. 41 ◽

Cited By ~ 2

Author(s):

Prabhjot Kaur ◽

Varun Garg, ◽

Palak Bawa ◽

Roopesh Sharma ◽

Sachin Kumar Singh ◽

...

Keyword(s):

Ex Vivo ◽

Entrapment Efficiency ◽

Stability Assessment ◽

Box Behnken Design ◽

Vesicle Size ◽

Drug Permeation ◽

Drug Retention ◽

Efficient Delivery ◽

Morphology Parameters

Objectives: The current work presents a formulation of curcumin-loaded transethosome (CRM-TE) in the form of a gel and its characterization.Methods: Thirteen formulations were prepared by varying the concentration of Phospholipon 90G as lipid, ethanol, and ratio of lipid: Span using Box- Behnken Design. The optimized formulation was characterized by vesicle size, entrapment efficiency, drug retention, drug permeation through skin, and morphology. Parameters of CRM-TE were compared to other vesicular systems that include liposomes, ethosomes, and transfersomes. Optimized CRM-TE was incorporated into gels, and comparative evaluation was performed. CRM-TE gel was kept at 5±3°C, 25±3°C, and 40±3°C for 180 days, further evaluated for entrapment efficacy and vesicle size.Results: CRM-TE showed 286.4 nm vesicle size, 61.2% entrapment efficiency, 19.8% drug retention, and 71.3% drug permeation at 24 h in the skin. It was found superior in terms of all the parameters as compared to other vesicular formulations. CRM-TE gel also exhibited best characteristics in terms of entrapment efficiency, drug retention, and drug permeation. CRM-TE gel exhibited better stability at 5±3°C in terms of vesicle size and entrapment efficiency as compared to other storage conditions.Conclusion: CRM-TE gel could offer efficient delivery of curcumin through topical route.

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DEVELOPMENT AND EVALUATION OF NANOEMULSION AS A CARRIER FOR TOPICAL DELIVERY SYSTEM BY BOX-BEHNKEN DESIGN

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2018.v11i8.26359 ◽

2018 ◽

Vol 11 (8) ◽

pp. 286

Author(s):

Pallavi M Chaudhari ◽

Madhavi A Kuchekar

Keyword(s):

Drug Release ◽

Ftir Spectroscopy ◽

Ex Vivo ◽

Topical Delivery ◽

Homogenization Method ◽

Permeation Rate ◽

Scanning Calorimetry ◽

Box Behnken Design ◽

Globule Size

Objective: The aim of this study was to develop a nanoemulsion for topical delivery. Methods: Topical nanoemulsion was prepared by homogenization method. Box-behnken design was utilized to study the effect of oil, surfactant and Co-surfactant, on droplet size, entrapment efficiency and drug release. Nabumetone a non-steroidal anti-inflammatory drug was incorporated in castor oil with Tween 80 and Polyethylene glycol 600 to form the nanoemulsion by homogenization method. The nanoemulsion was further subjected to different evaluation parameters and ex-vivo study. The crystalline nature of drug was confirmed by powder X-ray diffraction studies. Drug-excipient compatibility was confirmed by Fourier transform infrared (FTIR) spectroscopy, differential scanning calorimetry (DSC), respectively. Results: The average globule size of nabumetone-containing nanoemulsion decreased with decrease in concentration of oil and surfactant. Nanoemulsion was evaluated by pH, rheology, globule size, zeta potential, scanning electron microscopy, DSC, FTIR spectroscopy, and stability. In vitro drug release shows maximum 84.35% permeation rate through cellophane membrane and ex-vivo drug release shows 86.32% permeation rate through goat skin. Conclusion: Thus, the nanoemulsion formulated showed good results regarding topical delivery.

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Constant Voltage Iontophoresis Technique to Deliver Terbinafine via Transungual Delivery System: Formulation Optimization Using Box–Behnken Design and In Vitro Evaluation

Pharmaceutics ◽

10.3390/pharmaceutics13101692 ◽

2021 ◽

Vol 13 (10) ◽

pp. 1692

Author(s):

Anroop B. Nair ◽

Bandar E. Al-Dhubiab ◽

Jigar Shah ◽

Bapi Gorain ◽

Shery Jacob ◽

...

Keyword(s):

Low Voltage ◽

Ex Vivo ◽

Topical Therapy ◽

Nail Plate ◽

Drug Accumulation ◽

Constant Voltage ◽

Box Behnken Design ◽

Ex Vivo Permeation ◽

Transungual Delivery

Topical therapy of antifungals is primarily restricted due to the low innate transport of drugs through the thick multi-layered keratinized nail plate. The objective of this investigation was to develop a gel formulation, and to optimize and evaluate the transungual delivery of terbinafine using the constant voltage iontophoresis technique. Statistical analysis was performed using Box–Behnken design to optimize the transungual delivery of terbinafine by examining crucial variables namely concentration of polyethylene glycol, voltage, and duration of application (2–6 h). Optimization data in batches (F1–F17) demonstrated that chemical enhancer, applied voltage, and application time have influenced terbinafine nail delivery. Higher ex vivo permeation and drug accumulation into the nail tissue were noticed in the optimized batch (F8) when compared with other batches (F1–F17). A greater amount of terbinafine was released across the nails when the drug was accumulated by iontophoresis than the passive counterpart. A remarkably higher zone of inhibition was observed in nails with greater drug accumulation due to iontophoresis, as compared to the passive process. The results here demonstrate that the optimized formulation with low voltage iontophoresis could be a viable and alternative tool in the transungual delivery of terbinafine, which in turn could improve the success rate of topical nail therapy in onychomycosis.

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