Formulation, Optimization,and Ex-Vivo Evaluation of Novel Lipid Carriers for Enhanced Transdermal Delivery of Hydroquinone

2020 ◽  
Vol 12 ◽  
Author(s):  
Shivani Verma ◽  
Sukhjinder Kaur ◽  
Lalit Kumar
Keyword(s):  
Ex Vivo ◽  
Skin Permeation ◽  
Topical Delivery ◽  
Gelling Agent ◽  
Minimum Size ◽  
Prolonged Release ◽  
Freeze Dried ◽  
Ft Ir ◽  
Ir Analysis ◽  
Skin Retention

Background: HQ is used for hyper-pigmentation treatment using conventional creams and gels. These formulations show various disadvantages like poor skin permeation, allergic reactions, and repeated use decreasing patient compliance. Objectives: The present work involved formulation, statistical optimization, and characterization of nanostructured lipid carriers (NLCs) for efficient topical delivery of hydroquinone (HQ) for hyperpigmentation treatment. Methods: The NLCs were optimized exploring Box–Behnken design (BBD) using three independent variables and two dependent variables. Formulation having the minimum size and maximum drug entrapment was considered as optimized formulation. Optimized formulation was evaluated for drug release followed by its freeze-drying. The freeze-dried formulation was subjected to differential scanning calorimetry (DSC) analysis, X-raydiffraction (XRD) analysis, and Fourier transform-infrared spectroscopy (FT-IR) analysis. Furthermore, NLCs based gel was prepared by using Carbopol 934 as a gelling agent. NLCs based gel was evaluated for skin permeation, skin retention, and skin distribution (through confocal microscopic analysis) using pig ear skin. Results: Optimized NLCs showed smaller particle size [(271.9 ± 9) nm], high drug entrapment [(66.4 ± 1.2) %], tolerable polydispersity index (PDI) (0.221 ± 0.012), and zeta potential [(-25.9± 1.2) mV]. The FT-IR analysis revealed excellent compatibility between HQ and other excipients. The Carbopol 934 gel containing NLCs showed high transdermal flux [(163 ± 16.2) μg/cm2/h], permeability coefficient (0.0326 ± 0.0016), and skin permeation enhancement ratio (3.7 ± 0.4) compared to marketed cream of HQ. The results of confocal microscopic (CLSM) analysis revealed the accumulation of optimized NLCs in the lower epidermal layers of skin. Conclusion: NLCs based gel was considered effective in the topical delivery of HQ to treat hyper-pigmentation due high skin permeation, skin retention, and prolonged release of HQ.

scholarly journals Topical Delivery of Meloxicam using Liposome and Microemulsion Formulation Approaches

Pharmaceutics ◽  
2020 ◽  
Vol 12 (3) ◽  
pp. 282 ◽  
Author(s):  
Julia Zhang ◽  
Anna Froelich ◽  
Bozena Michniak-Kohn
Keyword(s):  
Transdermal Delivery ◽  
Oral Delivery ◽  
Ex Vivo ◽  
Skin Permeation ◽  
Entrapment Efficiency ◽  
Topical Delivery ◽  
Onset Of Action ◽  
Promising Alternative ◽  
Inflammatory Drugs ◽  
Systemic Onset

The aim of this study is to develop, characterize and compare conventional liposome, deformable liposome (transfersome) and microemulsion formulations as potential topical delivery systems for meloxicam. Liposomes were characterized in terms of vesicle size, zeta potential and entrapment efficiency. For microemulsions, particle size, electrical conductivity and viscosity studies were performed to assess the structure of the investigated systems. An ex vivo skin permeation study has been conducted to compare these formulations. The dermal and transdermal delivery of meloxicam using these formulations can be a promising alternative to conventional oral delivery of non-steroidal anti-inflammatory drugs (NSAIDs) with enhanced local and systemic onset of action and reduced side effects.

scholarly journals Nutritional, phytochemical and antioxidant evaluation and FT-IR analysis of freeze dried extracts of Ecballium elaterium fruit juice from three localities

2016 ◽  
Vol 36 (4) ◽  
pp. 646-655 ◽  
Author(s):  
Samir FELHI ◽  
Hafedh HAJLAOUI ◽  
Marwa NCIR ◽  
Sana BAKARI ◽  
Naourez KTARI ◽  
...  
Keyword(s):  
Fruit Juice ◽  
Freeze Dried ◽  
Antioxidant Evaluation ◽  
Ft Ir ◽  
Ir Analysis

Development and Evaluation of Ketoconazole Loaded Nano-sponges for Topical Drug Delivery

2018 ◽  
Vol 11 (4) ◽  
pp. 4154-4162
Author(s):  
Harshal A. Pardeshi ◽  
Makarand S Gambhire ◽  
Kishore N. Gujar ◽  
Aniket A Vaidhya
Keyword(s):  
Drug Delivery ◽  
Antifungal Activity ◽  
Drug Release ◽  
Ex Vivo ◽  
Skin Permeation ◽  
Controlled Drug Release ◽  
Topical Drug Delivery ◽  
Molar Ratios ◽  
Skin Targeting ◽  
Skin Retention

Beta-cyclodextrin nanosponges (NS) based hydrogel had been studied as a topical delivery of ketoconazole (KTZ) for effective eradication of cutaneous fungal infection. The purpose of the present study was to develop KTZ loaded NS for topical drug delivery with skin targeting to minimizing the adverse side effects and providing a controlled release. The four types of NS were synthesized by varying the molar ratios of β-cyclodextrin (β-CD) to diphenylcarbonate (DPC) as a cross linker viz. 1:2, 1:4, 1:6, and 1:8. The KTZ loaded NS shows particle size 274.6-367 nm and high loading efficacy was obtained, FTIR, DSC, XRD studies confirmed the complexation of KTZ with NS. Hydrogel were evaluated comparatively with commercial product with respect to physicochemical properties, ex-vivo skin permeation and skin retention on human cadaver skin and antifungal activity. Ex-vivo study of KTZ-NS hydrogel exhibited controlled drug release up to 8 hrs whereas skin retention studies show avoidance of the systemic uptake and better accumulative uptake of the drug compared to marketed formulation. The zone of inhibition of KTZ-NS hydrogel was higher in comparison with commercial formulation against Candida albicans. These results indicate that the KTZ-NS is having controlled drug release, potential of skin targeting with enhanced antifungal activity.

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 Microemulsion System for Topical Delivery of Thai Mango Seed Kernel Extract: Development, Physicochemical Characterisation and Ex Vivo Skin Permeation Studies

Molecules ◽  
2014 ◽  
Vol 19 (11) ◽  
pp. 17107-17129 ◽  
Author(s):  
Jiraporn Leanpolchareanchai ◽  
Karine Padois ◽  
Françoise Falson ◽  
Rapepol Bavovada ◽  
Pimolpan Pithayanukul
Keyword(s):  
Ex Vivo ◽  
Skin Permeation ◽  
Topical Delivery ◽  
Microemulsion System ◽  
Seed Kernel ◽  
Mango Seed Kernel ◽  
Permeation Studies ◽  
Physicochemical Characterisation ◽  
Mango Seed

scholarly journals Nanostructured Non-Ionic Surfactant Carrier-Based Gel for Topical Delivery of Desoximetasone

2021 ◽  
Vol 22 (4) ◽  
pp. 1535
Author(s):  
Parinbhai Shah ◽  
Benjamin Goodyear ◽  
Nirali Dholaria ◽  
Vinam Puri ◽  
Bozena Michniak-Kohn
Keyword(s):  
Drug Delivery ◽  
Skin Diseases ◽  
Skin Permeation ◽  
Topical Delivery ◽  
Gelling Agent ◽  
Oral Drug ◽  
Ionic Surfactant ◽  
Content Uniformity ◽  
Drug Bioavailability ◽  
Drug Content

Psoriasis is a chronic autoimmune skin disease impacting the population globally. Pharmaceutical products developed to combat this condition commonly used in clinical settings are IV bolus or oral drug delivery routes. There are some major challenges for effectively developing new dosage forms for topical use: API physicochemical nature, the severity of the disease state, and low bioavailability present challenges for pharmaceutical product developers. For non-severe cases of psoriasis, topical drug delivery systems may be preferred or used in conjunction with oral or parenteral therapy to address local symptoms. Elastic vesicular systems, termed “niosomes”, are promising drug delivery vehicles developed to achieve improved drug delivery into biological membranes. This study aimed to effectively incorporate a corticosteroid into the niosomes for improving the drug bioavailability of desoximetasone, used to treat skin conditions via topical delivery. Niosomes characterization measurements were drug content, pH, spreadability, specific gravity, content uniformity, rheology, and physicochemical properties. Formulations used a topical gelling agent, Carbomer 980 to test for in vitro skin permeation testing (IVPT) and accelerated stability studies. The developed niosomal test gel provided approximately 93.03 ± 0.23% to 101.84 ± 0.11% drug content with yield stresses ranging from 16.12 to 225.54 Pa. The permeated amount of desoximetasone from the niosomal gel after 24 h was 9.75 ± 0.44 µg/cm2 compared to 24.22 ± 4.29 µg/cm2 released from the reference gel tested. Furthermore, a drug retention study compared the test gel to a reference gel, demonstrating that the skin retained 30.88 ng/mg of desoximetasone while the reference product retained 26.01 ng/mg. A controlled drug release profile was obtained with a niosomal formulation containing desoximetasone for use in a topical gel formulation showing promise for potential use to treat skin diseases like psoriasis.

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

Improved in vitro Release and ex vivo Permeation of Zotepine as Microemulsion Gel Formulation through Transdermal Application

2021 ◽  
Vol 14 (1) ◽  
pp. 5343-5352
Author(s):  
Akhila Keshoju ◽  
Dinesh Suram ◽  
Chandra Mouli Golla ◽  
Nagaraj B
Keyword(s):  
Ex Vivo ◽  
In Vitro Release ◽  
Gelling Agent ◽  
Prolonged Release ◽  
Rat Skin ◽  
Skin Delivery ◽  
Ex Vivo Permeation ◽  
Vitro Release ◽  
Microemulsion Gel

Zotepine is atypical antipsychotic drug with poor oral bioavailability due to first-pass metabolism and poor aqueous solubility. The objective of the current investigation was preparation and ex vivo characterization of Zotepine (ZT) loaded microemulsion (ZT-ME) and microemulsion gel (ZT-MEG) for enhanced transdermal delivery.  ZT-ME formulation was prepared with 7.5% oleic acid, 30% w/v of Tween80 and 30%w/v of absolute ethanol as oil, surfactant and cosurfactant, respectively. Optimized ZT-ME formulation was selected and converted to ZT-MEG using carbopol as gelling agent. ZT-ME and ZT-MEG subjected to in vitro release and ex vivo permeation studies through rat skin, comparison with ZT coarse suspension (ZT-CS). ZT-ME formulation showed desirable physicochemical properties and stable with dilution stress. Prepared ZT-MEG formulation has showed better rheological behaviour and good spreadability. ZT-ME and ZT-MEG showed prolonged release compared with ZT-CS formulation over 24 h. ZT-ME and ZT-MEG exhibited 5-folds and 3.5-folds in permeation through rat skin compared with ZT-CS formulation. Overall, ZT-MEG formulation could be considered as an alternative delivery approach for enhanced skin delivery. 

scholarly journals Formulation Consideration and Skin Retention-Permeation Study of Insitu Nanogel Containing Dimethylfumarate for Treatment of Psoriasis

2021 ◽  
pp. 248-261
Author(s):  
Deepa Patel ◽  
Sneha Patel
Keyword(s):  
Skin Permeation ◽  
Crosslinking Agent ◽  
Topical Delivery ◽  
Surface Epithelium ◽  
Permeation Study ◽  
Skin Uptake ◽  
Full Factorial ◽  
Retention Study ◽  
Skin Retention ◽  
32 Full Factorial Design

Aims and Objective: to develop and evaluate an insitu nanogel formulation containing dimethylfumarate for targeted topical delivery therapy of psoriasis. Study Design: 32 full factorial design Place and Duration of Study: Department of Pharmaceutics, Parul Institute of Pharmacy and Research, Parul University, Vadodara, between 2016 to 2019. Methodology: Nanogel were formulated by chemical cross linked gel method using Polyvinyl alcohol and Hyaluronic acid (1:5) ratio using Glutaraldehyde (GA) (25 %w/v) and Hydrochloric acid (HCl) (6%v/v) as a crosslinking agent and catalyst. Dimethylfumarate loaded nanogel were clear and showed physicochemical parameters desired for topical delivery and stability. Results: The Permeation profile of dimethylfumarate through rat skin from selected nanogel formulation exhibited highest skin uptake. The Micoscopic observations indicated that the optimized nanogel had n significant effect on the microscopic structure of the sin and epithelial cells appered mostly unchanged. The surface epithelium lining and the granular cellular structure of the skin were totally intact. The developed Nanogel may be a potential drug delivery vehicle for targeted topical delivery of dimethylfumarate in the treatment of psoriasis. Conclusion: As per drug retention study the highest amount of drug retained on the skin and lowest amount of drug permeate to the skin. Hence it was observed that there was no significant correlation between skin retention and skin permeation study.

scholarly journals Efficacy of Gelling Agents on the In-vitro Release and Physical Properties of Loxoprofen Sodium Gel Containing Ultra Elastic Vesicles

2019 ◽  
Vol 9 (04) ◽  
pp. 671-677
Author(s):  
Huda S. Kadhium ◽  
Nidhal K. Maraie
Keyword(s):  
Skin Permeation ◽  
Skin Irritation ◽  
In Vitro Release ◽  
Gelling Agent ◽  
Burst Release ◽  
Prolonged Release ◽  
Gelling Agents ◽  
Loxoprofen Sodium

Objective: Preparation of a topical prolong release gel for loxoprofen sodium using optimized nano-sized transfersome dispersion using different gelling agents with in vitro and in vivo evaluation in comparison to the marketed gel prepared by a conventional method. Method: The optimum nano transfersome dispersion containing 5% egg lecithin (as an oil phase) 1% span 60 (as an emulsifying agent) was converted into a gel using different gelling agents including carbopol 974p, carbopol 940, carbopol 934 and hydroxyl propyl methylcellulose (HPMC K100) at ratio of (1:1). Each prepared gel was then evaluated in vitro to determine the homogenisity, consistency, spreadability, viscosity, and in vitro drug release as well as skin permeation test, human skin irritation test, and in vivo effectiveness. Result: The selected gel formula (TG3) showed best homogenisity, consistency and spreadability as well as it produced initial burst release of 60.3% (within 1 hour) followed by the prolonged release of 95.4% continued for 6 hours. In addition, the optimum gel formula (TG3) has shown remarkable prolong release, which was significantly higher than the marketed gel (loxonin® gel 1%) without any sign of skin irritation with better effectiveness Conclusion: This work succeeded in preparing topical gel for loxoprofen sodium using carbopol 974p as gelling agent and utilizing ultra elastic lipid vesicles (transfersomes) with prolong release that reduces dose frequency and improves patient compliance

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