scholarly journals Feasibility of binary composition in development of nanoethosomal glycolic vesicles of triamcinolone acetonide using Box-behnken design: in vitro and ex vivo characterization

2016 ◽  
Vol 45 (6) ◽  
pp. 1123-1131 ◽  
Author(s):  
Nida Akhtar ◽  
Anurag Verma ◽  
Kamla Pathak
2016 ◽  
Vol 2016 ◽  
pp. 1-9 ◽  
Author(s):  
Ma Da ◽  
Kenneth K. W. Li ◽  
Kevin C. Chan ◽  
Ed X. Wu ◽  
David S.H. Wong

There is increasing use of the vitreous cavity as a reservoir for drug delivery. We study the intraocular migration and distribution of triamcinolone acetonide (TA) after injection into silicone oil tamponade agent during and after vitrectomy surgeryex vivo(pig eye) andin vitro(glass bottle). Forex vivoassessment, intraocular migration of TA was imaged using real-time FLASH MRI scans and high-resolution T2W imaging and thein vitromodel was monitored continuously with a video camera. Results of theex vivoexperiment showed that the TA droplet sank to the interface of silicone oil and aqueous almost immediately after injection and remained inside the silicone oil bubble for as long as 16 minutes. Thein vitroresults showed that, after the shrinkage of the droplet, TA gradually precipitated leaving only a lump of whitish crystalline residue inside the droplet for about 100 minutes. TA then quickly broke the interface and dispersed into the underlying aqueous within 15 seconds, which may result in a momentary increase of local TA concentration in the aqueous portion and potentially toxic to the retina. Our study suggests that silicone oil may not be a good candidate as a drug reservoir for drugs like TA.


Author(s):  
Parul A. Ittadwar ◽  
Prashant K. Puranik

<p><strong>Objective: </strong>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.</p><p><strong>Methods: </strong>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.</p><p><strong>Results: </strong>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 <em>ex vivo</em> and <em>in-vitro</em> permeation of the complex showed improved permeation for complex than the drug. The <em>in vitro</em> 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.</p><strong>Conclusion: </strong>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.


2021 ◽  
Vol 2021 ◽  
pp. 1-13
Author(s):  
Saeed Ebrahimi ◽  
Reza Mahjub ◽  
Rasool Haddadi ◽  
Seyed Yaser Vafaei

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


Author(s):  
Prabhjot Kaur ◽  
Varun Garg, ◽  
Palak Bawa ◽  
Roopesh Sharma ◽  
Sachin Kumar Singh ◽  
...  

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.


Author(s):  
Pallavi M Chaudhari ◽  
Madhavi A Kuchekar

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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