Development and Evaluation of Nanoemulsion as a Carrier for Topical Delivery System by Box-Behnken Design

Chaudhari, Pallavi M.; Kuchekar, Madhavi A

doi:10.22159/ajpcr.2018.v11i8.26359

Cited by 25 publications

(20 citation statements)

References 7 publications

(7 reference statements)

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“…Some recently approved commercial topical formulations of 5-FU (0.5%) include Carac ® ; Sanofi, Gentilly, France [ 20 ], Fluoroplex 1% 5-FU solution (Allergan, Inc., Irvine, CA, USA), creams (Efudex ® , Valeant Pharmaceuticals, Bridgewater, NJ, USA) and a 0.5% microsphere-based cream (Carac ® , Valeant Pharmaceuticals) [ 21 ]. A report has suggested that commercially available topical products offer the demerit of low retention time at the delivery site that results in inadequate skin permeation along with skin irritation reactions, such as dryness, redness, swelling, and burning pain of the upper layer of skin [ 22 , 23 ].…”

Section: Introductionmentioning

confidence: 99%

Chitosan-Coated 5-Fluorouracil Incorporated Emulsions as Transdermal Drug Delivery Matrices

et al. 2021

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The purpose of the present study was to develop emulsions encapsulated by chitosan on the outer surface of a nano droplet containing 5-fluorouracil (5-FU) as a model drug. The emulsions were characterized in terms of size, pH and viscosity and were evaluated for their physicochemical properties such as drug release and skin permeation in vitro. The emulsions containing tween 80 (T80), sodium lauryl sulfate, span 20, and a combination of polyethylene glycol (PEG) and T20 exhibited a release of 88%, 86%, 90% and 92%, respectively. Chitosan-modified emulsions considerably controlled the release of 5-FU compared to a 5-FU solution (p < 0.05). All the formulations enabled transportation of 5-FU through a rat’s skin. The combination (T80, PEG) formulation showed a good penetration profile. Different surfactants showed variable degrees of skin drug retention. The ATR-FTIR spectrograms revealed that the emulsions mainly affected the fluidization of lipids and proteins of the stratum corneum (SC) that lead to enhanced drug permeation and retention across the skin. The present study concludes that the emulsions containing a combination of surfactants (Tween) and a co-surfactant (PEG) exhibited the best penetration profile, prevented the premature release of drugs from the nano droplet, enhanced the permeation and the retention of the drug across the skin and had great potential for transdermal drug delivery. Therefore, chitosan-coated 5-FU emulsions represent an excellent possibility to deliver a model drug as a transdermal delivery system.

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Section: Introductionmentioning

confidence: 99%

Chitosan-Coated 5-Fluorouracil Incorporated Emulsions as Transdermal Drug Delivery Matrices

et al. 2021

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“…To determine the pH of the gel formulation, 1 g of gel was dissolved in 25 mL of distilled water, followed by a pH measurement using a pH meter (Accumet meter 21039, Denver Instruments, USA) at 25 ± 1 • C. For instrument calibration, buffer solutions with known pH (3, 7, and 9) were employed. At room temperature, rheological characteristics of gel formulations were evaluated using a Brookfield viscometer (RVTD, USA) fitted with a UL-adapter [30]. With a #64 spindle, measurements were taken at a constant (40 rpm) as well as variable (10-120 rpm) shear speeds.…”

Section: Physico-chemical and Rheological Characterization Of Methotrexate Nanoemulsion Gelmentioning

confidence: 99%

Olive Oil Based Methotrexate Loaded Topical Nanoemulsion Gel for the Treatment of Imiquimod Induced Psoriasis-like Skin Inflammation in an Animal Model

Rashid

Bashir

Naseem

et al. 2021

Biology

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Psoriasis, a chronic inflammatory illness, is on the rise and is linked to several other life-threatening diseases. The primary goal of this study was to create a nanoemulsion gel loaded with methotrexate and olive oil (MTX NEG). The formulation was evaluated for physicochemical characterization, entrapment efficiency, drug release kinetics, skin permeation studies and stability tests. In addition, the efficacy of MTX NEG against psoriasis was tested using imiquimod-induced psoriasis in a rat model. The final optimized MTX NEG was developed with a particle size of 202.6 ± 11.59 nm and a PDI of 0.233 ± 0.01, with a 76.57 ± 2.48% average entrapment efficiency. After 20 h, the release kinetics predicted a 72.47% drug release at pH 5.5. FTIR findings demonstrated that the optimized MTX NEG formulation effectively fluidized both the epidermis and dermis of the skin, potentially increasing drug permeability and retention. The application of Tween 80 and PEG 400, on the other hand, significantly enhanced these effects, as these are well known penetration enhancers. After 24 h, an average of 70.78 ± 5.8 μg/cm2 of methotrexate was permeated from the nanoemulsion gel with a flux value of 2.078 ± 0.42 μg/cm2/h, according to permeation measurements. Finally, in vivo experiments on rabbit skin revealed that the increased skin penetration of methotrexate-loaded nanoemulsion gel was not due to structural alterations in intercellular lipid layers in the stratum corneum. In vivo antipsoriatic studies on rats revealed that MTX NEG produced a PASI decrease that was extremely similar and even better than the 91% reduction seen in the MTX tablet group. According to the pharmacokinetic profile, Cmax was 8.5 μg/mL, Tmax was 12 h, and t1/2 was 15.5 ± 2.37 h. These findings reinforce that MTX-NEG based on olive oil could be a possible treatment for psoriasis and could decrease the remission of psoriasis-like symptoms.

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“…Nanoemulsions [1] are high solubilizing and drug protection features have the potential to deliver proteins as well as other new (or traditional) active drug compounds. Although authors have suggested using nanoemulsion formulations for inflammation [2][3][4][5][6][7]. Budesonide (16,17-butylidenebis(oxy)-11,21-dihydroxypregna-1,4diene-3,20-dione) is a synthetic glucocorticoid steroid used in the treatment of asthma and an inflammatory bowel disease [9].…”

Section: Research Articlementioning

confidence: 99%

Optimization and Solubilization Study of Nanoemulsion Budesonide and Constructing Pseudoternary Phase Diagram

Puppala

2019

Asian J Pharm Clin Res

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Objective: The aim of the present study was to formulate and optimize budesonide nanoemulsions for targeting inflammation.Methods: Budesonide is only found in individuals that have used or taken this drug. It is a glucocorticoid used in the management of asthma, the treatment of various skin disorders, and allergic rhinitis. The exact mechanism of the action of budesonide in the treatment of Crohn’s disease is not fully understood. However, being a glucocorticosteroid, budesonide has a high local anti-inflammatory effect. The formulation was optimized for different components and the solubility study for the oil in surfactant and cosurfactant mix ratio was optimized using ternary phase diagram.Results: The surfactant mix ratio was optimized as 1:3 where the maximum concentration of the oil has solubilized and the nanoemulsion area was increased.Conclusion: Budesonide nanoemulsion for targeting inflammation and the pseudoternary phase diagram for the solubility studies and the components of different phases were optimized and achieved through this study.

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Development and Evaluation of Nanoemulsion as a Carrier for Topical Delivery System by Box-Behnken Design

Cited by 25 publications

References 7 publications

Chitosan-Coated 5-Fluorouracil Incorporated Emulsions as Transdermal Drug Delivery Matrices

Chitosan-Coated 5-Fluorouracil Incorporated Emulsions as Transdermal Drug Delivery Matrices

Olive Oil Based Methotrexate Loaded Topical Nanoemulsion Gel for the Treatment of Imiquimod Induced Psoriasis-like Skin Inflammation in an Animal Model

Optimization and Solubilization Study of Nanoemulsion Budesonide and Constructing Pseudoternary Phase Diagram

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