Skin Delivery and Irritation Potential of Phenmetrazine as a Candidate Transdermal Formulation for Repurposed Indications

Background: In this study, a liposomal gel based on a pH-gradient method was used to increase the skin-layer retention of monocrotaline (MCT) for topical administration. Methods: Using the Box-Behnken design, different formulations were designed to form liposome suspensions with optimal encapsulation efficiency (EE%) and stability factor (KE). In order to keep MCT in liposomes and accumulate in skin slowly and selectively, MCT liposome suspensions were engineered into gels. Results: A pH-gradient method was used to prepare liposome suspensions. The optimal formulation of liposome suspensions (encapsulation efficiency: 83.10 ± 0.21%) was as follows: MCT 12 mg, soybean phosphatidyl choline (sbPC) 200 mg, cholesterol (CH) 41 mg, vitamin E (VE) 5 mg, and citric acid buffer solution (CBS) 4.0 10 mL (pH 7.0). The final formulation of liposomal gels consisted of 32 mL liposome suspensions, 4.76 mL deionized water, 0.40 g Carbopol-940, 1.6 g glycerol, 0.04 g methylparaben, and a suitable amount of triethanolamine for pH value adjustment. The results of in vitro drug release showed that MCT in liposomal gels could be released in 12 h constantly in physiological saline as a Ritger-Peppas model. Compared with plain MCT in gel form, liposomal MCT in gel had higher skin retention in vitro. Conclusion: In this study, liposomal gels were formed for greater skin retention of MCT. It is potentially beneficial for reducing toxicities of MCT by topical administration with liposomal gel.

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FORMULATION AND IN VITRO, IN VIVO EVALUATION OF PRONIOSOMAL GEL OF NEOMYCIN SULPHATE

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2019v11i2.30614 ◽

2019 ◽

pp. 156-163

Author(s):

AMOL SHETE ◽

PRIYANKA THORAT ◽

RAJENDRA DOIJAD ◽

SACHIN SAJANE

Keyword(s):

Phase Separation ◽

Skin Irritation ◽

Entrapment Efficiency ◽

Separation Method ◽

Gelling Agent ◽

In Vivo Evaluation ◽

Skin Delivery ◽

Span 60

Objective: The objectives of present investigation were to prepare and evaluate proniosomes of neomycin sulphate (NS) by coacervation phase separation method by using sorbitan monostearate (span 60) and lecithin as a surfactant to increase the penetration through the skin and study the effect of concentration of the same. Methods: Proniosomes of neomycin sulphate (NS) were prepared by coacervation phase separation method by using span 60 and lecithin. The effect of concentration of span 60 and lecithin was studied by factorial design. The prepared proniosomes were converted to gel by using carbopol as a gelling agent. The prepared formulations were evaluated for entrapment efficiency, in vitro drug diffusion, in vitro antibacterial activity and in vivo skin irritation test etc. Results: All Formulation showed the percentage entrapment efficiency in the range 38.31±0.05% to 77.96±0.06%, good homogeneity and gel was easily spreadable with minimal of shear. Optimized formulation showed enhanced rate of diffusion in vitro, increase in zone of inhibition against staphylococcus aureus, no skin irritation and showed good stability. Conclusion: The results of present study indicates that proniosomal gel formulated by using combination of span 60, Lecithin, cholesterol can be used to enhance skin delivery of NS because of excellent permeation of drug. Developed proniosomal gel formulation was promising carrier for NS

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Camelina lipid droplets as skin delivery system promotes wound repair by enhancing the absorption of hFGF2

International Journal of Pharmaceutics ◽

10.1016/j.ijpharm.2021.120327 ◽

2021 ◽

Vol 598 ◽

pp. 120327

Author(s):

Hongtao Gao ◽

Fawei Wang ◽

Xingli Hu ◽

Yulin Li ◽

Yuan Zhang ◽

...

Keyword(s):

Delivery System ◽

Lipid Droplets ◽

Wound Repair ◽

Skin Delivery

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Positively Charged Lipid as Potential Tool to Influence the Fate of Ethosomes

Applied Sciences ◽

10.3390/app11157060 ◽

2021 ◽

Vol 11 (15) ◽

pp. 7060

Author(s):

Antonia Mancuso ◽

Maria Chiara Cristiano ◽

Massimo Fresta ◽

Daniele Torella ◽

Donatella Paolino

Keyword(s):

Cell Model ◽

Human Keratinocytes ◽

Skin Delivery ◽

Physico Chemical ◽

Cell Mortality ◽

Mean Size ◽

A Cell ◽

Negative Surface ◽

Cytotoxic Studies

Ethosomes® are one of the main deformable vesicles proposed to overcome the stratum corneum. They are composed of lecithin, ethanol and water, resulting in round vesicles characterized by a narrow size distribution and a negative surface charge. Taking into account their efficiency to deliver drugs into deeper skin layers, the current study was designed to evaluate the influence of different lipids on the physico-chemical features of traditional ethosomes in the attempt to influence their fate. Three lipids (DOPE, DSPE and DOTAP) were used for the study, but only DOTAP conferred a net positive charge to ethosomes, maintaining a narrow mean size lower than 300 nm and a good polydispersity index. Stability and in vitro cytotoxic studies have been performed using Turbiscan Lab analysis and MTT dye exclusion assay, respectively. Data recorded demonstrated the good stability of modified ethosomes and a reasonable absence of cell mortality when applied to human keratinocytes, NCTC 2544, which are used as a cell model. Finally, the best formulations were selected to evaluate their ability to encapsulate drugs, through the use of model compounds. Cationic ethosomes encapsulated oil red o and rhodamine b in amounts comparable to those recorded from conventional ethosomes (over 50%). Results recorded from this study are encouraging as cationic ethosomes may open new opportunities for skin delivery.

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Physico-Chemical Characterization and Biopharmaceutical Evaluation of Lipid-Poloxamer-Based Organogels for Curcumin Skin Delivery

Frontiers in Pharmacology ◽

10.3389/fphar.2019.01006 ◽

2019 ◽

Vol 10 ◽

Author(s):

Aryane Alves Vigato ◽

Samyr Machado Querobino ◽

Naially Cardoso de Faria ◽

Ana Carolina Bolela Bovo Candido ◽

Lizandra Guidi Magalhães ◽

...

Keyword(s):

Chemical Characterization ◽

Skin Delivery ◽

Physico Chemical

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Ethosomes for skin delivery of ammonium glycyrrhizinate: In vitro percutaneous permeation through human skin and in vivo anti-inflammatory activity on human volunteers

Journal of Controlled Release ◽

10.1016/j.jconrel.2005.04.007 ◽

2005 ◽

Vol 106 (1-2) ◽

pp. 99-110 ◽

Cited By ~ 169

Author(s):

Donatella Paolino ◽

Giuseppe Lucania ◽

Domenico Mardente ◽

Franco Alhaique ◽

Massimo Fresta

Keyword(s):

Human Skin ◽

Inflammatory Activity ◽

Skin Delivery ◽

Percutaneous Permeation ◽

Human Volunteers ◽

Anti Inflammatory

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Bioadhesive liquid crystal systems for octyl methoxycinnamate skin delivery

Journal of Molecular Liquids ◽

10.1016/j.molliq.2021.117450 ◽

2021 ◽

pp. 117450

Author(s):

Alice Haddad do Prado ◽

Jonatas Lobato Duarte ◽

Leonardo Delello Di Filippo ◽

Francesca Damiani Victorelli ◽

Marcia Carvalho de Abreu Fantini ◽

...

Keyword(s):

Liquid Crystal ◽

Skin Delivery

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Lamellar Lyotropic Liquid Crystal Phases as a Carrier for Skin Delivery of Morus alba Stem Extract

Key Engineering Materials ◽

10.4028/www.scientific.net/kem.901.67 ◽

2021 ◽

Vol 901 ◽

pp. 67-72

Author(s):

Chein Yhirayha ◽

Sakchai Wittaya-Areekul ◽

Tasana Pitaksuteepong

Keyword(s):

Liquid Crystal ◽

Biological Activities ◽

Polarized Light ◽

Water Extract ◽

Skin Penetration ◽

Morus Alba ◽

Lyotropic Liquid Crystal ◽

Mixed Surfactant ◽

Skin Delivery ◽

Stem Extract

Morus alba stem extract possesses several biological activities. However, skin delivery of the extract is limited by the stratum corneum. In this study, lamellar lyotropic liquid crystal (LLC) was investigated for the potential application in the skin delivery of M. alba stem extract. The four formulations were developed and incorporated with M. alba stem extract at 3% w/w. These formulations were stored at room temperature in light-protected containers for 3 months. The optical pattern under polarized light microscope, viscosity and remaining of the extract were determined. The skin penetration enhancing property of the formulations was investigated using excised porcine ear skin model. The results showed that all formulations remained stable after 3-month storage. The two formulations exhibiting good penetration enhancing properties were F3 consisting of PEG-7 glyceryl cocoate/n-Dodecane/Water/extract (55.29/19.40/22.31/3.00 %w/w) and F4 consisting of mixed Surfactant/n-Dodecane/Water/extract (48.50/4.85/43.65/3.00 %w/w). The mixed surfactant composed of PEG-7 glyceryl cocoate/PEG-40 hydrogenated castor oil/Glyceryl oleate (40/33.24/26.76 %w/w). It can be concluded that the lamellar LLC formulations developed in this study can be used as a carrier for delivering of M. alba stem extract. The components of the formulations which play important roles are the oil and the surfactant.

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Physical characterisation and stability study of formulated Chromolaena odorata gel

Current Drug Delivery ◽

10.2174/1567201818666210419114809 ◽

2021 ◽

Vol 18 ◽

Author(s):

Qurratul Ain Zakirah Mohd Zamram ◽

Hannis Fadzillah Mohsin ◽

Mashani Mohamad Mohamad ◽

Nurul Aqmar Mohamad Nor Hazalin ◽

Khuriah Abdul Hamid

Keyword(s):

High Performance ◽

Skin Diseases ◽

Loss Modulus ◽

Viscosity Index ◽

Stability Study ◽

Wound Management ◽

Flavonoid Compound ◽

Chromolaena Odorata ◽

Skin Delivery ◽

Materials Used

Aim: Formulating topical products for skin delivery has always been a challenge for pharmaceutical scientists to fulfil good formulation criteria. Despite the challenges, gel-based drug delivery offers some advantages such that it is non-invasive, painless, avoidance of the first-pass metabolism and has satisfactory patient compliance. Objectives: In this study, Chromolaena odorata gel and quercetin gel (bioactive flavonoid compound) were successfully formulated and compared with placebo and conventional wound aid gel. The chromatographic profilling was conducted to screen the presence of phytoconstituents. Subsequently, all formulated gels were subjected to physical characteristic and stability study. Methods: Reverse Phase High-Performance Liquid Chromatography (RP-HPLC) of C.odorata methanolic leaves extract shows a distinct compound separation at retention time 8.4min to 34.8 min at 254nm. All gels were characterised by evaluating their rheological properties including storage modulus, loss modulus and plastic viscosity. Besides, texture analysis was performed to measure the gels’ firmness, consistency, cohesiveness, and viscosity index. Results: From the observation, C. odorata gel demonstrated better spreadability as compared to the other gels, which acquired less work and favourable to be applied onto the skin. Moreover, C. odorata gel showed no changes in organoleptic properties and proven to be stable after 30 days of accelerated stability study at 40°C ± 2°C with relative humidity (RH) of 75%± 5%. Conclusion: C. odorata gel has shown to be stable, reflecting the combination of materials used in the formulation, which did not degrade throughout the study. This work suggests the potential of this gel as a vehicle to deliver the active ingredients of C. odorata to the skin, which can be further explored as a topical application in antimicrobial wound management or other skin diseases study.

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