scholarly journals Influence of Chemical Enhancers and Iontophoresis on the In Vitro Transdermal Permeation of Propranolol: Evaluation by Dermatopharmacokinetics

Pharmaceutics ◽  
2018 ◽  
Vol 10 (4) ◽  
pp. 265 ◽  
Author(s):  
María Calatayud-Pascual ◽  
María Sebastian-Morelló ◽  
Cristina Balaguer-Fernández ◽  
M. Delgado-Charro ◽  
Alicia López-Castellano ◽  
...  
Keyword(s):  
Oleic Acid ◽  
Stratum Corneum ◽  
Model Compound ◽  
Skin Permeation ◽  
Chemical Enhancer ◽  
Chemical Enhancers ◽  
Transdermal Permeation ◽  
Topical Bioavailability ◽  
Current Densities

The aims of this study were to assess, in vitro, the possibility of administering propranolol transdermally and to evaluate the usefulness of the dermatopharmacokinetic (DPK) method in assessing the transport of drugs through stratum corneum, using propranolol as a model compound. Four chemical enhancers (decenoic and oleic acid, laurocapram, and R-(+)-limonene) and iontophoresis at two current densities, 0.25 and 0.5 mA/cm2 were tested. R-(+)-limonene, and iontophoresis at 0.5 mA/cm2 were proven to be the most efficient in increasing propranolol transdermal flux, both doubled the original propranolol transdermal flux. Iontophoresis was demonstrated to be superior than the chemical enhancer because it allowed faster delivery of the drug. The DPK method was sufficiently sensitive to detect subtle vehicle-induced effects on the skin permeation of propranolol. The shorter duration of these experiments and their ability to provide mechanistic information about partition between vehicle and skin and diffusivity through skin place them as practical and potentially insightful approach to quantify and, ultimately, optimize topical bioavailability.

scholarly journals EFFECT OF MENTHOL ON THE TRANSDERMAL PERMEATION OF ACECLOFENAC FROM MICROEMULSION FORMULATION

2019 ◽  
pp. 117-122
Author(s):  
Abdul Baquee Ahmed ◽  
Gouranga Das
Keyword(s):  
Droplet Size ◽  
Skin Permeation ◽  
Peak Height ◽  
Skin Permeability ◽  
Permeability Barrier ◽  
Microemulsion Formulation ◽  
Transdermal Permeation ◽  
Ir Studies ◽  
Ft Ir

Objective: The aim of this investigation was to enhance the transdermal permeation of aceclofenac (ACF) from microemulsion formulation using menthol as a natural permeation enhancer. Methods: Microemulsion containing 2% w/v of ACF was prepared by a titration method with different concentration of oil, surfactant and co-surfactant. The prepared microemulsion was evaluated for droplet size, viscosity, pH and in vitro skin permeation studies. Menthol at 3-8% w/w was added to the selected microemulsion formulation and their effect on skin permeation was evaluated across rat epidermis using modified Keshary-Chien diffusion cell. The Fourier transform infrared spectroscopy (FT-IR) was performed to understand the regulation action of menthol in the skin permeability barrier. Results: The average droplet size of the microemulsion was found to be 89.4±2.12 to 175.2±3.10 nm. The transdermal flux of the microemulsion containing 8% w/w menthol showed 2.9 fold increases in transdermal flux of ACF compared with the formulation without menthol. Result of FT-IR studies showed decrease in peak height of the symmetric and asymmetric C-H stretching vibrations may be because of the extraction of the stratum corneum (SC) lipids and the alteration of the skin permeability barrier. Conclusion: This result suggests that menthol significantly enhanced the transdermal permeation of ACF and may be an effective natural penetration enhancer for transdermal delivery of the drug.

Oleic Acid Vesicles as a new Approach for Transdermal Delivery of Econazole Nitrate: Development, Characterization, and In-vivo Evaluation in Wistar rats

2020 ◽  
Vol 15 ◽  
Author(s):  
Shivani Verma ◽  
Puneet Utreja
Keyword(s):  
Oleic Acid ◽  
Antifungal Activity ◽  
Side Effects ◽  
Fungal Infection ◽  
Wistar Rats ◽  
Skin Permeation ◽  
Cutaneous Candidiasis ◽  
Econazole Nitrate

Background:: Cutaneous candidiasis is a deep-seated skin fungal infection that is most commonly observed in immunocompromised patients. This fungal infection is conventionally treated with various formulations like gels and creams which are having different side effects and least therapeutic efficacy. Hence, it becomes necessary to develop a novel carrier system for the treatment of this deep-seated skin fungal infection. Econazole nitrate is the most widely used antifungal for the treatment of cutaneous candidiasis, therefore, in present research work we developed and evaluated econazole nitrate loaded oleic acid vesicles for treatment of cutaneous candidiasis through transdermal route. Methods:: Econazole nitrate loaded oleic acid vesicles were prepared by thin-film hydration and characterized for drug entrapment, vesicle size, zeta potential, polydispersity index (PDI), Fourier Transform-infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), X-ray diffraction (XRD) analysis. Furthermore, the oleic acid vesicular gel was evaluated for ex-vivo skin permeation/retention and in-vitro and in-vivo antifungal activity in Wistar rats. Results:: Econazole nitrate loaded oleic acid vesicles showed high encapsulation of drug (74.76 ± 3.0%), acceptable size (373.4 ± 2.9 nm), and colloidal characteristics (PDI = 0.231 ± 0.078, zeta potential = -13.27 ± 0.80 mV). The oleic acid vesicular gel showed high skin permeation (Transdermal flux = 61.98 ± 2.45 μg/cm2/h), skin retention (35.90 ± 2.06%), in-vitro, and in-vivo antifungal activity compared to marketed cream (EcodermR) of econazole nitrate for a prolonged period of time (4 days). Conclusion:: Developed econazole nitrate loaded oleic acid vesicles could be used effectively in the treatment of cutaneous candidiasis with minimization of side effects of econazole nitrate with increased therapeutic efficacy.

scholarly journals Use of an In Vitro Skin Parallel Artificial Membrane Assay (Skin-PAMPA) as a Screening Tool to Compare Transdermal Permeability of Model Compound 4-Phenylethyl-Resorcinol Dissolved in Different Solvents

Pharmaceutics ◽  
2021 ◽  
Vol 13 (11) ◽  
pp. 1758
Author(s):  
Bálint Sinkó ◽  
Vivien Bárdos ◽  
Dániel Vesztergombi ◽  
Szabina Kádár ◽  
Petra Malcsiner ◽  
...  
Keyword(s):  
Human Skin ◽  
Model Compound ◽  
Ex Vivo ◽  
Early Stage ◽  
Skin Permeation ◽  
Polar Compounds ◽  
Formulation Development ◽  
Artificial Membrane ◽  
Pig Skin

Absorption through the skin of topically applied chemicals is relevant for both formulation development and safety assessment, especially in the early stages of development. However, the supply of human skin is limited, and the traditional in vitro methods are of low throughput. As an alternative, an artificial membrane-based Skin Parallel Artificial Membrane Permeability Assay (Skin-PAMPA) has been developed to mimic the permeability through the stratum corneum. In this study, this assay was used to measure the permeability of a model compound, 4-phenylethyl-resorcinol (PER), dissolved in 13 different solvents that are commonly used in cosmetic formulation development. The study was performed at concentrations close to the saturated solution of PER in each solvent to investigate the maximum thermodynamic potential of the solvents. The permeability of PER in selected solvents was also measured on ex vivo pig skin for comparison. Pig ear skin is an accepted alternative model of human skin. The permeability coefficient, which is independent of the concentration of the applied solution, showed a good correlation (R2 = 0.844) between the Skin-PAMPA and the pig skin permeation data. Our results support the use of the Skin-PAMPA to screen the suitability of different solvents for non-polar compounds at an early stage of formulation development.

Vehicle effects on in vitro skin permeation of and stratum corneum affinity for model drugs caffeine and testosterone

1993 ◽  
Vol 100 (1-3) ◽  
pp. 41-47 ◽  
Author(s):  
F.P. Bonina ◽  
V. Carelli ◽  
G. Di Colo ◽  
L. Montenegro ◽  
E. Nannipieri
Keyword(s):  
Stratum Corneum ◽  
Skin Permeation ◽  
In Vitro Skin Permeation

scholarly journals In Vitro Skin Retention of Crisaborole after Topical Application

Pharmaceutics ◽  
2020 ◽  
Vol 12 (6) ◽  
pp. 491
Author(s):  
Adriana Fantini ◽  
Anna Demurtas ◽  
Sara Nicoli ◽  
Cristina Padula ◽  
Silvia Pescina ◽  
...  
Keyword(s):  
Stratum Corneum ◽  
Skin Permeation ◽  
Skin Penetration ◽  
Skin Layer ◽  
Hair Follicles ◽  
Relative Distribution ◽  
Phosphodiesterase 4 ◽  
Receptor Compartment ◽  
Drug Partitioning

Crisaborole, a nonsteroidal phosphodiesterase 4 inhibitor, represents the first nonsteroidal medication approved for the treatment of atopic dermatitis in over a decade. In this work, crisaborole skin permeation and retention was studied in vitro from a 2% ointment using porcine skin as barrier. Crisaborole was also characterized in terms of thermal behavior, solubility, and logP. Control experiments were performed also on tape stripped skin to clarify the role of stratum corneum in drug partitioning and permeation across the skin. The results obtained indicate that crisaborole accumulates into the skin in considerable amounts after application of a topical lipophilic ointment. Crisaborole shows more affinity for the dermis compared to the epidermis despite its relatively high value of partition coefficient; stratum corneum analysis revealed a low affinity of the drug for this skin layer. Skin penetration across hair follicles or sebaceous glands can be a reason for the high dermis retention and is worth further investigation. The comparison with data obtained from a solution in acetonitrile suggests that the formulation plays a certain role in determining the relative distribution of crisaborole in the skin layers and in the receptor compartment.

scholarly journals Oleic Acid Nanovesicles of Minoxidil for Enhanced Follicular Delivery

Medicines ◽  
2018 ◽  
Vol 5 (3) ◽  
pp. 103 ◽  
Author(s):  
Pawan Kumar ◽  
Shailendra Singh ◽  
Vandana Handa ◽  
Himanshu Kathuria
Keyword(s):  
Oleic Acid ◽  
Side Effects ◽  
Confocal Microscopy ◽  
Drug Release ◽  
Zeta Potential ◽  
Skin Permeation ◽  
Entrapment Efficiency ◽  
Hair Follicles ◽  
In Vitro Drug Release

Current topical minoxidil (MXD) formulations involve an unpleasant organic solvent which causes patient incompliance in addition to side effects in some cases. Therefore, the objective of this work was to develop an MXD formulation providing enhanced follicular delivery and reduced side effects. Oleic acid, being a safer material, was utilized to prepare the nanovesicles, which were characterized for size, entrapment efficiency, polydispersity index (PDI), zeta potential, and morphology. The nanovesicles were incorporated into the emugel Sepineo® P 600 (2% w/v) to provide better longer contact time with the scalp and improve physical stability. The formulation was evaluated for in vitro drug release, ex vivo drug permeation, and drug deposition studies. Follicular deposition of the vesicles was also evaluated using a differential tape stripping technique and elucidated using confocal microscopy. The optimum oleic acid vesicles measured particle size was 317 ± 4 nm, with high entrapment efficiency (69.08 ± 3.07%), narrow PDI (0.203 ± 0.01), and a negative zeta potential of −13.97 ± 0.451. The in vitro drug release showed the sustained release of MXD from vesicular gel. The skin permeation and deposition studies revealed superiority of the prepared MXD vesicular gel (0.2%) in terms of MXD deposition in the stratum corneum (SC) and remaining skin over MXD lotion (2%), with enhancement ratios of 3.0 and 4.0, respectively. The follicular deposition of MXD was 10-fold higher for vesicular gel than the control. Confocal microscopy also confirmed the higher absorption of rhodamine via vesicular gel into hair follicles as compared to the control. Overall, the current findings demonstrate the potential of oleic acid vesicles for effective targeted skin and follicular delivery of MXD.

scholarly journals Formulation and In Vitro Evaluation of Ufasomes for Dermal Administration of Methotrexate

2012 ◽  
Vol 2012 ◽  
pp. 1-8 ◽  
Author(s):  
Arvind Sharma ◽  
Sandeep Arora
Keyword(s):  
Oleic Acid ◽  
Fatty Acid ◽  
Skin Permeation ◽  
In Vitro Release ◽  
Principal Component ◽  
Topical Administration ◽  
Synovial Joint ◽  
Scanning Calorimetry ◽  
Dermal Administration

Dermal drug delivery system that is required to localizes methotrexate (MTX) in the synovial joint is needed to treat inflammation in rheumatoid arthritis (RA). The present investigation aims at exploring the potential of fatty acid vesicles for the topical delivery of methotrexate. Vesicles were prepared by film hydration method using oleic acid as a fatty acid principal component. Developed vesicles were characterized for size, size distribution, shape, in vitro release, pH dependent, and storage stability. Interaction between MTX and oleic acid was investigated using differential scanning calorimetry. The MTX amount permeated through rat skin was three- to fourfold higher using oleic acid compared to those from plain drug solution or carbopol gel. At the end of the skin permeation assay using ufasomes, up to 50% of the administered dose was found in the skin. These results suggest that methotrexate encapsulated in oleic acid vesicles may be of value for the topical administration of MTX in the treatment of psoriasis.

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