scholarly journals 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

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

scholarly journals LORNOXICAM-LOADED NANOSPONGES FOR CONTROLLED ANTI-INFLAMMATORY EFFECT: IN VITRO/IN VIVO ASSESSMENT

2020 ◽  
pp. 217-223
Author(s):  
SEHAM M. SHAWKY ◽  
MAHA K. A. KHALIFA ◽  
HEBA A. EASSA
Keyword(s):  
Skin Permeation ◽  
Skin Irritation ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Topical Delivery ◽  
Inflammatory Activity ◽  
Carboxymethyl Cellulose Sodium ◽  
Anti Inflammatory

Objective: To design a controlled topical delivery system of lornoxicam (LX) in order to enhance skin permeation and treatment efficacy. Nanosponges were selected as a novel carrier for this purpose. Methods: Nanosponges were formulated via the emulsion solvent evaporation method using ethyl cellulose (polymer) and polyvinyl alcohol (surfactant). Nanosponge dispersions were characterized for colloidal properties, entrapment efficiency and in vitro release study. The nanosponge formulation (LS1) was then incorporated into carboxymethyl cellulose sodium hydrogels and evaluated for pH, viscosity and in vitro drug release. Skin irritation was evaluated, and anti-inflammatory activity was assessed via rat hind paw edema method. Results: Nanosponges were in the nano-sized range and attained a uniform round shape with a spongy structure. LS1exhibited the highest LX release after 6 h, so it was incorporated as hydrogel. Formulated hydrogels showed acceptable physicochemical parameters (pH, drug content and rheological properties). Skin irritation testing proved LX-loaded nanosponge hydrogel formulation (G1) to be non-irritant. In vivo study revealed an enhanced anti-inflammatory activity of G1 for 6 h (p<0.001). Conclusion: The developed nanosponge hydrogel is an efficient nanocarrier for improved and controlled topical delivery of LX.

Optimized Preparation of Capsaicin-Loaded Nanoparticles Gel by Box-Behnken Design

2014 ◽  
Vol 1061-1062 ◽  
pp. 359-368 ◽  
Author(s):  
Mei Ling Tang ◽  
Li Hua Chen ◽  
Dong Sheng Zhou ◽  
Wei Feng Zhu ◽  
Yong Mei Guan ◽  
...  
Keyword(s):  
Skin Permeation ◽  
Skin Irritation ◽  
Morphological Characteristics ◽  
Entrapment Efficiency ◽  
Box Behnken Design ◽  
Irritation Test ◽  
Predicted Values ◽  
Skin Irritation Test

A three-factor three-level Box-Behnken design(BBD) was employed to optimize capsaicin-loaded nanoparticles(Cap-NPs), and its properties in vitro and in vivo were evaluated. Particle size, morphological characteristics, entrapment efficiency of Cap-NPs were investigated respectively by Zetasizer, H7000 TEM and HPLC. Release, skin permeation and skin irritation test were investigated on mouse and rabbits. The predicted values of Cap-NPs were 94.50±6.33% for entrapment efficiency(EE) and 170.30±7.81 nm for particle mean diameter(PMD) under optimal conditions which were 346.33 bar (homogenization pressure, X1), 4.67 min(homogenization time, X2), and 15421.42 rpm (shear rate, X3). The in vitro permeation study showed that capsaicin permeability in NPs-gel was a 2.80-fold greater flux values than conventional ointment after 24 h. Cap-NPs-gel produce no observable skin irritation in rabbits within 72h. The optimized Cap-NPs-gel would be a good candidate for transdermal delivery.

Studies with Emulsion Containing trans-resveratrol: in vitro Release Profile and ex vivo Human Skin Permeation

2015 ◽  
Vol 12 (2) ◽  
pp. 157-165 ◽  
Author(s):  
Priscila de Almeida ◽  
Michele Alves ◽  
Hudson Polonini ◽  
Stephane Calixto ◽  
Tiago Braga Gomes ◽  
...  
Keyword(s):  
Human Skin ◽  
Ex Vivo ◽  
Skin Permeation ◽  
In Vitro Release ◽  
Release Profile ◽  
Vitro Release

FORMULATION AND OPTIMIZATION OF TOPICAL NANOEMULSION BASED GEL OF MOMETASONE FUROATE USING 32 FULL FACTORIAL DESIGN

INDIAN DRUGS ◽  
2021 ◽  
Vol 58 (06) ◽  
pp. 19-29
Author(s):  
Bhupendra G. Prajapati ◽  
◽  
Malay Jivani ◽  
Himanshu Paliwal ◽  
Keyword(s):  
Ex Vivo ◽  
Skin Permeation ◽  
In Vitro Release ◽  
Tween 80 ◽  
Stability Study ◽  
Mometasone Furoate ◽  
Gelling Agent ◽  
Topical Formulation ◽  
Topical Gel

Mometasone furoate (MF) is a glucocorticoid prodrug that faces the problem of poor aqueous solubility. Nanoemulsion-based topical gel of MF was formulated to enhance its solubility and potential of treating skin conditions. The selection of oil, surfactant and co-surfactant was done based on their solubility with the drug. The nanoemulsion was prepared using rose oil as the oil phase. Tween 80 and Transcutol P were used as surfactant and co-surfactant and they were blended in different ratios (1:0, 1:1, 2:1 and 3:1 w/w). The pseudo ternary diagrams were developed using these excipients and formulations exhibiting considerable nanoemulsion region were selected. The formulations were optimized by using Design Expert software for the globule size and cumulative percent release. The nanoemulsion formulations were characterized for in vitro release and stability study. The optimized nanoemulsions consisting of 2 % w/w oil, 30 % w/w Smix (Surfactant: Co-surfactant) and 67.9 % w/w water were consolidated into Carbopol 940 gelling agent to prepare three nanoemulsion-based gel formulations or nanoemulgels (NEG1-NEG3). Nanoemulgels were evaluated for their stability and ex vivo permeation of MF. The outcomes suggested that skin permeation of MF from all the nanoemulgel formulations was significantly enhanced as compared to the marketed mometasone furoate topical formulation.

scholarly journals Enhancement of Curcumin Anti-Inflammatory Effect via Formulation into Myrrh Oil-Based Nanoemulgel

Polymers ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 577 ◽  
Author(s):  
Wafaa E. Soliman ◽  
Tamer M. Shehata ◽  
Maged E. Mohamed ◽  
Nancy S. Younis ◽  
Heba S. Elsewedy
Keyword(s):  
Ex Vivo ◽  
Skin Permeation ◽  
In Vitro Release ◽  
Aqueous Solubility ◽  
Delivery Methods ◽  
Anti Cancer ◽  
Permeation Studies ◽  
Anti Inflammatory

Background: Curcumin (Cur) possesses a variety of beneficial pharmacological properties including antioxidant, antimicrobial, anti-cancer and anti-inflammatory activities. Nevertheless, the low aqueous solubility and subsequent poor bioavailability greatly limits its effectiveness. Besides, the role of myrrh oil as an essential oil in treating inflammatory disorders has been recently demonstrated. The objective of the current investigation is to enhance Cur efficacy via developing Cur nanoemulgel, which helps to improve its solubility and permeability, for transdermal delivery. Methods: The formulated preparations (Cur gel, emulgel and nanoemulgel) were evaluated for their physical appearance, spreadability, viscosity, particle size, in vitro release and ex vivo drug permeation studies. The in vivo anti-inflammatory activity was estimated using the carrageenan-induced rat hind paw edema method. Results: The formulated Cur-loaded preparations exhibited good physical characteristics that were in the acceptable range of transdermal preparations. The release of Cur from gel, emulgel and nanoemulgel after 12 h was 72.17 ± 3.76, 51.93 ± 3.81 and 62.0 ± 3.9%, respectively. Skin permeation of Cur was significantly (p < 0.05) improved when formulated into nanoemulgel since it showed the best steady state transdermal flux (SSTF) value (108.6 ± 3.8 µg/cm2·h) with the highest enhancement ratio (ER) (7.1 ± 0.2). In vivo anti-inflammatory studies proved that Cur-loaded nanoemulgel displayed the lowest percent of swelling (26.6% after 12 h). Conclusions: The obtained data confirmed the potential of the nanoemulgel dosage form and established the synergism of myrrh oil and Cur as an advanced anti-inflammatory drug.

scholarly journals The Optimization of a Dimenhydrinate Transdermal Patch Formulation Based on the Quantitative Analysis of In Vitro Release Data by DDSolver through Skin Penetration Studies

2021 ◽  
Vol 89 (3) ◽  
pp. 33
Author(s):  
Bazigha K. Abdul Rasool ◽  
Amira A. Mohammed ◽  
Yasmein Y. Salem
Keyword(s):  
Quantitative Analysis ◽  
Ex Vivo ◽  
Skin Irritation ◽  
In Vitro Release ◽  
Control Sample ◽  
Skin Penetration ◽  
Penetration Enhancers ◽  
Release Data ◽  
Skin Irritation Test

Dimenhydrinate is an over-the-counter medication that is used to relieve nausea, vomiting, and vertigo caused by motion sickness. It has a short elimination half-life, possibly due to its first-pass metabolism. The current study aimed to prepare and evaluate new transdermal formulations of dimenhydrinate to prolong the drug’s release and improve its cutaneous permeation. First, the patches were fabricated and evaluated to determine their properties. The results were statistically investigated and considered significant at the p < 0.05 level. Additionally, the quantitative analysis of the drug-release data and kinetic modeling was performed by using the DDSolver software to decide the candidate formula dependably. The effect of the penetration enhancers on the permeability of dimenhydrinate from the selected patch was then studied ex vivo compared to the control sample, and the patch’s safety was evaluated in rabbits, using the skin-irritation test.

scholarly journals Formulation and Evaluation of Minoxidil Gel Using Acrylamide/Sodium Acryloyldimethyl taurate copolymer for Alopecia areata

2018 ◽  
Vol 10 (01) ◽  
Author(s):  
Shailendra Kumar Singh ◽  
Pawan Kumar ◽  
Deepak Kumar Jindal ◽  
Vandana Handa ◽  
Jyoti Bilonia
Keyword(s):  
Drug Release ◽  
Alopecia Areata ◽  
Ex Vivo ◽  
Skin Permeation ◽  
In Vitro Release ◽  
Chronic Inflammatory Disease ◽  
Effective Dosage ◽  
World Population ◽  
Drug Content

Alopecia areata is a common, chronic inflammatory disease, characterized by patchy hair loss on the scalp, affecting about 2.1% of world population. Presently, minoxidil has been used for treatment of alopecia as topical lotion, but associated with many drawbacks like systemic side effects and low contact time with skin. Therefore, in the present work, minoxidil gel was prepared using a novel copolymer, Sepineo P 600 to overcome these drawbacks. The prepared gel was characterized for pH, drug content, viscosity, spreadability, skin adhesivity, occlusivity, in vitro drug release, ex vivo skin permeation, stability and finally for skin corrosivity. The drug content of the finalized gel was found to be 99.80 ± 0.82%. The formulation showed good spreadability, occlusivity, adhesiveness and viscosity. In vitro release studies showed that the drug release from prepared gel followed matrix release pattern as compared to lotion. Mathematical modelling of the drug release data suggested Higuchi release model. The formulated minoxidil gel was found to be non-corrosive and stable when subjected to accelerate as well as real time stability studies. Overall, the minoxidil gel formulation was suitable for skin application and can be an effective dosage form for the treatment of Alopecia areata.

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

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.

scholarly journals FORMULATION AND OPTIMIZATION OF QUERCETIN LOADED NANOSPONGES TOPICAL GEL: EX VIVO, PHARMACODYNAMIC AND PHARMACOKINETIC STUDIES

2019 ◽  
pp. 156-165
Author(s):  
Y. SARAH SUJITHA ◽  
Y. INDIRA MUZIB
Keyword(s):  
Particle Size ◽  
Ex Vivo ◽  
Skin Permeation ◽  
Hydroxypropyl Methylcellulose ◽  
Entrapment Efficiency ◽  
Diffusion Method ◽  
Pharmacokinetic Studies ◽  
Topical Gel

Objective: Quercetin is therapeutically hampered because of its poor solubility. The present investigation was aimed to prepare quercetin loaded nanosponges topical gel to enhance the solubility and efficacy of the drug. Methods: Quercetin nanosponges were prepared by emulsion solvent diffusion method. Developed nanosponges optimized by particle size, SEM, entrapment efficiency, FT-IR, DSC, P-XRD, In vitro studies. The optimized formulation of nanosponges was loaded into a topical gel and it was characterized by ex-vivo, in vivo Pharmacodynamic and kinetic studies. Results: The particle size and zeta potential of optimized nanosponges were found to be 188.3 nm and-0.1mV. Surface morphology was studied using SEM Analysis which showed tiny sponge-like structure and entrapment efficiency was found to be 96.5 %. In vitro drug release of optimized nanosponges was found to be 98.6% for 7hours. Optimized nanosponges entrapped gel was prepared by using carbopol 934 and hydroxypropyl methylcellulose as gelling agents. The prepared nanogels were homogenous and ex-vivo skin permeation studies of the optimized nanosponges gel was found to be 98.1% for 5 h, quercetin loaded nanosponges has shown higher skin permeation efficiency (18.4µg/cm2±2.1) compared to pure quercetin gel. The pharmacokinetic and pharmacodynamic studies showed that the quercetin loaded nanosponges has shown more effective when compared to marketed formulation. Conclusion: Quercetin loaded nanosponges gel has shown a significant increase in activity (p<0.05) compared to the marketed formulation (Voveran Emulgel).

scholarly journals Development and In Vitro/In Vivo Evaluation of pH-Sensitive Polymeric Nanoparticles Loaded Hydrogel for the Management of Psoriasis

Nanomaterials ◽  
2021 ◽  
Vol 11 (12) ◽  
pp. 3433
Author(s):  
Muhammad Imran Asad ◽  
Dildar Khan ◽  
Asim ur Rehman ◽  
Abdelhamid Elaissari ◽  
Naveed Ahmed
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Ex Vivo ◽  
Skin Irritation ◽  
Topical Formulation ◽  
Sustained Drug Release ◽  
In Vivo Evaluation ◽  
Ex Vivo Permeation ◽  
Pasi Score

Methotrexate (MTX), the gold standard against psoriasis, poses severe problems when administered systemically viz increased toxicity, poor solubility and adverse reactions. Hence, a topical formulation of MTX for the management of psoriasis can be an effective approach. The present study aimed to develop an MTX based nanoparticle-loaded chitosan hydrogel for evaluating its potential efficacy in an imiquimod-induced psoriatic mice model. MTX-NPs loaded hydrogel was prepared and optimized using the o/w emulsion solvent evaporation method. Particle size, zeta potential, entrapment efficiency, in vitro drug release, ex vivo permeation, skin irritation and deposition studies were performed. Psoriatic Area and Severity Index (PASI) score/histopathological examinations were conducted to check the antipsoriatic potential of MTX-NPs loaded hydrogel using an imiquimod (IMQ)-induced psoriatic model. Optimized MTX-NPs showed a particle size of 256.4 ± 2.17 nm and encapsulation efficiency of 86 ± 0.03%. MTX-NPs loaded hydrogel displayed a 73 ± 1.21% sustained drug release in 48 h. Ex vivo permeation study showed only 19.95 ± 1.04 µg/cm2 of drug permeated though skin in 24 h, while epidermis retained 81.33% of the drug. A significant decrease in PASI score with improvement to normalcy of mice skin was observed. The developed MTX-NPs hydrogel displayed negligible signs of mild hyperkeratosis and parakeratosis, while histopathological studies showed healing signs of mice skin. So, the MTX-NPs loaded hydrogel can be a promising delivery system against psoriasis.

Sign in / Sign up

Export Citation Format

Share Document