scholarly journals An Investigation of the Influence of PEG 400 and PEG-6-Caprylic/Capric Glycerides on Dermal Delivery of Niacinamide

Polymers ◽  
2020 ◽  
Vol 12 (12) ◽  
pp. 2907
Author(s):  
Yanling Zhang ◽  
Majella E. Lane ◽  
David J. Moore
Keyword(s):  
Skin Permeation ◽  
Ternary Systems ◽  
Pharmaceutical Products ◽  
Porcine Skin ◽  
Peg 400 ◽  
Skin Delivery ◽  
Dermal Delivery ◽  
Binary And Ternary Systems ◽  
Skin Retention

Polyethylene glycols (PEGs) and PEG derivatives are used in a range of cosmetic and pharmaceutical products. However, few studies have investigated the influence of PEGs and their related derivatives on skin permeation, especially when combined with other solvents. Previously, we reported niacinamide (NIA) skin permeation from a range of neat solvents including propylene glycol (PG), Transcutol® P (TC), dimethyl isosorbide (DMI), PEG 400 and PEG 600. In the present work, binary and ternary systems composed of PEGs or PEG derivatives combined with other solvents were investigated for skin delivery of NIA. In vitro finite dose studies were conducted (5 μL/cm2) in porcine skin over 24 h. Higher skin permeation of NIA was observed for all vehicles compared to PEG 400. However, overall permeation for the binary and ternary systems was comparatively low compared with results for PG, TC and DMI. Interestingly, values for percentage skin retention of NIA for PEG 400:DMI and PEG 400:TC were significantly higher than values for DMI, TC and PG (p < 0.05). The findings suggest that PEG 400 may be a useful component of formulations for the delivery of actives to the skin rather than through the skin. Future studies will expand the range of vehicles investigated and also look at skin absorption and residence time of PEG 400 compared to other solvents.

scholarly journals Dermal Delivery Enhancement of Natural Anti-Ageing Compounds from Ocimum sanctum Linn. Extract by Nanostructured Lipid Carriers

Pharmaceutics ◽  
2020 ◽  
Vol 12 (4) ◽  
pp. 309
Author(s):  
Wantida Chaiyana ◽  
Songyot Anuchapreeda ◽  
Suvimol Somwongin ◽  
Pachabadee Marsup ◽  
Kuan-Han Lee ◽  
...  
Keyword(s):  
Zeta Potential ◽  
Droplet Size ◽  
Skin Permeation ◽  
In Vitro Release ◽  
Correlation Spectroscopy ◽  
Nanostructured Lipid Carriers ◽  
Ocimum Sanctum ◽  
Dermal Delivery ◽  
Skin Retention

This study aimed to develop nanodelivery systems for enhancing the Ocimum sanctum Linn. extract delivery into the skin. Rosmarinic acid (RA) was used as a marker for the quantitative determination of the extract by high-performance liquid chromatography. Nanostructured lipid carriers (NLC), nanoemulsion, liposome, and niosome, were developed and characterized for internal droplet size, polydispersity index (PDI), and zeta potential using photon correlation spectroscopy. Irritation properties of each formulations were investigated by hen’s egg test on the chorioallantoic membrane. In vitro release, skin permeation, and skin retention are determined. NLC was suggested as the most suitable system since it enhances the dermal delivery of RA with the significant skin retention amount of 27.1 ± 1.8% (p < 0.05). Its internal droplet size, PDI, and zeta potential were 261.0 ± 5.3 nm, 0.216 ± 0.042, and −45.4 ± 2.4 mV, respectively. RA released from NLC with a sustained release pattern with the release amount of 1.29 ± 0.15% after 24 h. NLC induced no irritation and did not permeate through the skin. Therefore, NLC containing O. sanctum extract was an attractive dermal delivery system that was safe and enhanced dermal delivery of RA. It was suggested for further used as topical anti-ageing products.

scholarly journals Topical Delivery of 3-O-ethyl l-ascorbic Acid from Complex Solvent Systems

2020 ◽  
Vol 88 (2) ◽  
pp. 19
Author(s):  
Fotis Iliopoulos ◽  
A. S. M. Monjur Al Hossain ◽  
Bruno C. Sil ◽  
David J. Moore ◽  
Robert A. Lucas ◽  
...  
Keyword(s):  
Ascorbic Acid ◽  
Propylene Glycol ◽  
Isopropyl Alcohol ◽  
Skin Permeation ◽  
Isopropyl Myristate ◽  
Medium Chain Triglycerides ◽  
Porcine Skin ◽  
Skin Delivery ◽  
Solvent Systems

3-O-ethyl l-ascorbic acid (EA), an ether derivative of Vitamin C, is widely used in skincare formulations. Previously, we reported the effects of neat solvents on EA percutaneous absorption and observed that 0.6–7.5% of the applied EA was delivered through the skin over 24 h. In this work, we designed complex formulations using combinations of solvents that may act synergistically and examined their impact on EA permeation in porcine skin in vitro under finite dose conditions. Binary combinations of propylene glycol (PG) with propylene glycol monolaurate (PGML) were effective in enhancing skin permeation of EA compared with individual solvents (p < 0.05). Combining PGML with 1,2-hexanediol (HEX) did not result in significantly higher EA permeation compared with the neat solvents (p > 0.05). Addition of the volatile solvent isopropyl alcohol (IPA) to PG solutions also did not improve EA skin delivery compared with neat PG. Ternary solvent systems containing PG:PGML were subsequently prepared by the addition of a lipophilic solvent, either isopropyl myristate (IPM), medium-chain triglycerides (MCT) or isostearyl isostearate (ISIS). The optimum vehicle, PG:PGML:IPM, promoted up to 70.9% skin delivery of EA. The PG:PGML:ISIS vehicles also promoted EA permeation across the skin, but to a significantly lesser extent than the IPM-containing vehicles. No enhancement of EA delivery was noted for the PG:PGML:MCT mixtures. These results will inform the development of targeted formulations for EA in the future.

Improving Topical Skin Delivery of Monocrotaline Via Liposome Gel-based Nanosystems

2019 ◽  
Vol 16 (10) ◽  
pp. 940-950 ◽  
Author(s):  
Jiandong Yu ◽  
Zhi Chen ◽  
Yan-zhi Yin ◽  
Chaoyuan Tang ◽  
Enying Hu ◽  
...  
Keyword(s):  
Gradient Method ◽  
Encapsulation Efficiency ◽  
Ph Value ◽  
Topical Administration ◽  
Ph Gradient ◽  
Stability Factor ◽  
Buffer Solution ◽  
Skin Delivery ◽  
Skin Retention

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.

Investigating the potential of Quercetin enthused nano lipoidal system for the management of dermatitis

2021 ◽  
pp. 6516-6526
Author(s):  
Deepti Dwivedi ◽  
Shubham Pandey ◽  
Shafaque Asif ◽  
Vineet Awasthi ◽  
Gurjeet Kaur ◽  
...  
Keyword(s):  
Zeta Potential ◽  
Skin Permeation ◽  
Research Work ◽  
Entrapment Efficiency ◽  
Laser Scanning Microscopy ◽  
Polydispersity Index ◽  
In Vivo Studies ◽  
Confocal Laser ◽  
Skin Retention

Objective: The present research work was undertaken to develop quercetin enthused nanolipoidal systems and its characterization. The objective was to investigate potential of prepared system in the management of DNCB induced dermatitis. Method: Nanolipoidal system was prepared in different combinations with quercetin, L-α phosphatidylcholine (SPC) and ethanol and characterized for particle size, polydispersity index (PDI), zeta potential, drug entrapment efficiency, percentage drug release, skin retention and skin permeation. Selected batches were further incorporated into Carbopol 934 base gel. The vesicles were in size range 324.19-359 nm while polydispersity index (PDI) ranges from 0.241-0.554 and for zeta potential, it was from -26.33 to -39.3 nm. Entrapment efficiency was from 23.77-94.68 %. Confocal laser scanning microscopy showed penetration depth of rhodamine enthused ethosome across rat skin up to 45.23 µm which was significantly higher than the rhodamine solution (10 µm). In dinitrochlorobenzene (DNCB) induced mice dermatitis model histopathology study showed a marked decrease in amount of inflammatory cell nucleus in mice treated with quercetin loaded ethosomal gel followed by 76.13% decrease in-ear swelling and ear mass respectively in morphology study. The conventional marketed formulation showed a nominal decrease in epidermal thickness. Further Primary irritation index was less than 0.4 indicating negligible irritation in all the groups. Results: The optimized formulation F6 with SPC and ethanol in the ratio of 20:80 displayed the highest drug content and entrapment efficiency of 94.68±1.14%. PDI was 0.241±0.11 and skin retention 7.7%. Batch F6 with vesicle size and zeta potential of 324.9±19 nm and -26.33 mV, respectively, was incorporated in Carbopol 934 base gel and the prepared gel was evaluated for morphology, spreadability, in vitro, ex vivo release study, and kinetics study and in vivo studies. Conclusion: The present study revealed that the developed ethosomal gel can be used for enhanced delivery of Quercetin via skin. The in vitro studies indicated that the gel serves as an efficient carrier for Quercetin. It showed its effectiveness in the management of dermatitis. Further, Quercetin loaded nanoethosomal gel formulation can be viewed as a promising drug delivery system for the management of dermatitis.

scholarly journals Transcutol® P Containing SLNs for Improving 8-Methoxypsoralen Skin Delivery

Pharmaceutics ◽  
2020 ◽  
Vol 12 (10) ◽  
pp. 973
Author(s):  
Giulia Pitzanti ◽  
Antonella Rosa ◽  
Mariella Nieddu ◽  
Donatella Valenti ◽  
Rosa Pireddu ◽  
...  
Keyword(s):  
Skin Permeation ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Skin Layer ◽  
Skin Permeability ◽  
Puva Therapy ◽  
Ultraviolet A ◽  
3T3 Fibroblasts ◽  
Skin Delivery

Topical psoralens plus ultraviolet A radiation (PUVA) therapy consists in the topical application of 8-methoxypsoralen (8-MOP) followed by the skin irradiation with ultraviolet A radiation. The employment of classical 8-MOP vehicles in topical PUVA therapy is associated with poor skin deposition and weak skin permeability of psoralens, thus requiring frequent drug administration. The aim of the present work was to formulate solid lipid nanoparticles (SLNs) able to increase the skin permeation of 8-MOP. For this purpose, the penetration enhancer Transcutol® P (TRC) was added to the SLN formulation. SLNs were characterized with respect to size, polydispersity index, zeta potential, entrapment efficiency, morphology, stability, and biocompatibility. Finally, 8-MOP skin diffusion and distribution within the skin layers was investigated using Franz cells and newborn pig skin. Freshly prepared nanoparticles showed spherical shape, mean diameters ranging between 120 and 133 nm, a fairly narrow size distribution, highly negative ζ potential values, and high entrapment efficiency. Empty and loaded formulations were almost stable over 30 days. In vitro penetration and permeation studies demonstrated a greater 8-MOP accumulation in each skin layer after SLN TRC 2% and TRC 4% application than that after SLN TRC 0% application. Finally, the results of experiments on 3T3 fibroblasts showed that the incorporation of TRC into SLNs could enhance the cellular uptake of nanoparticles, but it did not increase their cytotoxicity.

scholarly journals FORMULATION AND EVALUATION OF GEL CONTAINING ETHOSOMES ENTRAPPED WITH TRETINOIN

2018 ◽  
Vol 8 (5-s) ◽  
pp. 315-321
Author(s):  
Rakhi Mishra ◽  
Shradha Shende ◽  
Prabhat Kumar Jain ◽  
Vivek Jain
Keyword(s):  
Transdermal Delivery ◽  
Skin Permeation ◽  
Three Dimensional ◽  
Entrapment Efficiency ◽  
Brick Wall ◽  
Topical Formulation ◽  
Ir Studies ◽  
Skin Retention ◽  
Drug Solution

A skin disease, like acne, is very common and normally happens to everyone at least once in their lifetime. The structure of the stratum corneum is often compared with a brick wall, with corneocytes surrounded by the mortar of the intercellular lipid lamellae. One of the best options for successful drug delivery to the affected area of skin is the use of ethosomes which can be transported through the skin through channel-like structures. Tretinoin is a widely used retinoid for the topical treatment of acne, photo-aged skin, psoriasis and skin cancer which makes it a good candidate for topical formulation. Yet side effects, like redness, swelling, peeling, blistering and, erythema, in addition to its high lipophilicity make this challenging. Drug loaded ethosomes had been prepared using phospholipid and ethanol, were optimized and characterized for entrapment efficiency, vesicular size, shape, In-vitro skin permeation, skin retention, drug‐membrane component interaction and stability. The ethosomal formulation having 0.5 %w/v of phospholipid and 20 %v/v of ethanol (F2) showing the greatest entrapment efficiency (80.25±0.23) with small particle size (205.40±2.31nm) was selected for further skin permeation studies. The skin permeation and skin retention studies were performed on ethosomal formulation, liposomal formulation (0.5 %w/v of phospholipid without alcohol), hydroethanolic drug solution and phosphate buffer saline (pH7.4) drug solution. Among them, ethosomal formulation showed higher cumulative percentage of drug permeation (93.36±0.45%) and 8 hours than the other formulations. Scanning electron microscopy confirmed the three dimensional nature of ethosomes. Dynamic light scattering technique proved that the ethosomes has smaller vesicular size than the liposomes prepared without alcohol. FT‐IR studies revealed no interaction between the drug and membrane components. The ethosomal vesicles were incorporated in carbopol gel base and its anti‐acne was compared with the marketed gel. Our results suggest that the ethosomes are an efficient carrier for dermal and transdermal delivery of tretinoin. Keywords: Tretinoin, Ethosomes, Diffusion, Carbopol gels, Transdermal delivery.

scholarly journals FORMULATION AND EVALUATION OF TRANSDERMAL PATCHES OF METOPROLOL TARTRATE USING PERMEATION ENHANCERS OF NATURAL AND SYNTHETIC ORIGIN

2019 ◽  
pp. 317-323
Author(s):  
SHIKHA BAGHEL CHAUHAN ◽  
SUSHILA SAINI
Keyword(s):  
Moisture Absorption ◽  
Skin Permeation ◽  
Penetration Enhancers ◽  
Moisture Loss ◽  
Metoprolol Tartrate ◽  
Peg 400 ◽  
Transdermal Patches ◽  
Weight Variation ◽  
Basil Oil

Objective: Oral metoprolol tartrate has a short elimination half-life (2-3h) and low bioavailability undergoes extensive first-pass metabolism and frequent dosing. The aim of the present investigation was to formulate, develop and evaluate metoprolol tartrate transdermal patches using various synthetic and natural penetration enhancers. Methods: Enhancers used were eugenol, limonene, basil oil, urea and SLS (sodium lauryl sulphate). Polymer used was chitosan and PEG 400 used as a plasticizer. Transdermal Films were prepared by using solvent casting method. FTIR and DSC were studied to assess any interaction between the drug and polymers. Films were evaluated for Physico-chemical Characteristics like thickness, weight variation, folding endurance, moisture loss, moisture absorption and drug content. In vitro skin permeation studies were performed using Keshary chien cell For 24 h across rat skin. Results: Chitosan was found to be a suitable polymer for matrix formation. 3.5% w/w was used to optimize to formulate transdermal patches. 1.5% of total solution v/v lactic acid was used for dissolution of chitosan. 2.5%v/v of total solution PEG 400 was used to provide plasticity and smoothness to the patches. From the evaluation of patches formulation, F10 containing Basil oil as penetration enhancer in the concentration of 1.5% v/v was found to be best among all batches because of its consistent release rate For 24 h and extent of drug release was 85.20%. It can be concluded that naturally occurring volatile oils i.e., terpenes appear acceptable permeation enhancer and shows the best permeation across skin as indicated by high percutaneous enhancement ability. Conclusion: The developed transdermal patches are stable, non-irritating, and had increased efficacy of metoprolol and therefore had a good potential for hypertension treatment.

Effect of Various Nonionic Surfactants Incorporated in Liposomes on Dermal Delivery of Hydrophilic Compound

2014 ◽  
Vol 1060 ◽  
pp. 12-16
Author(s):  
Worranan Rangsimawong ◽  
Praneet Opanasopit ◽  
Theerasak Rojanarata ◽  
Tanasait Ngawhirunpat
Keyword(s):  
Nonionic Surfactants ◽  
Skin Permeation ◽  
Physicochemical Characteristic ◽  
Skin Penetration ◽  
Tween 20 ◽  
Negative Surface ◽  
Negative Surface Charge ◽  
Dermal Delivery ◽  
Hydrophilic Compound

Various surfactants-containing vesicles have been widely used as a carrier in drug delivery to enhance skin penetration of encapsulated therapeutic agents. The purpose of this study was to investigate the effect of nonionic surfactants-containing liposome vesicles on the penetration of hydrophilic compounds through the porcine skin. Ultradeformable liposomes composed of phosphatidylcholine (PC), cholesterol (Chol) and various surfactants e.g. Tween 20, Labrasol and Gelucire 44/14) were prepared as NaFI carrier. The physicochemical characteristic of liposomes and in vitro skin penetration were investigated. The particle size of surfactant-containing liposome vesicles showed smaller particle sizes (36 to 54 nm) than conventional liposome (CLs) and had negative surface charge. The EE% and LE% order of surfactants incorporated in liposome formulations were: Labrasol liposomes (LALs) > Gelucire 44/14 liposomes (GELs) > Tween20 liposomes (TWLs) > CLs. The flux of NaFI from ultradeformable liposomes was significantly higher than from CLs. Among various liposomes, Labrasol containing ultradeformable liposomes showed the highest skin permeation in 24 h, and their flux was significantly higher (p < 0.05) than the flux of CLs. The result suggests that the surfactant-containing liposomes were small and deformable vesicles due to incorporating of an edge activators. In addition, surfactants could act as a penetration enhancer to promote dermal delivery of NaFI.

scholarly journals The Effect of Cream and Gel Vehicles on the Percutaneous Absorption and Skin Retention of a New Eugenol Derivative With Antioxidant Activity

2021 ◽  
Vol 12 ◽  
Author(s):  
Edyta Makuch ◽  
Anna Nowak ◽  
Andrzej Günther ◽  
Robert Pełech ◽  
Łukasz Kucharski ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Steam Distillation ◽  
Skin Permeation ◽  
Biologically Active ◽  
Skin Permeability ◽  
Skin Accumulation ◽  
Radical Reduction ◽  
Skin Retention

The effect of cream and gel vehicles containing clove water on skin permeability was compared for a new eugenol derivative (eugenyl dichloroacetate—EDChA) with antioxidant activity. In vitro permeation experiments were conducted in a Franz cell with porcine skin. The cumulative mass and skin accumulation of EDChA were investigated and compared. The antioxidative capacity of the studied vehicles was determined by using the diphenylpicrylhydrazyl (DPPH) free radical reduction method. The antioxidant activity (evaluated with DPPH, ABTS, and the Folin–Ciocalteu methods) of the fluid that penetrated through the pig skin and of the fluid obtained after the skin extraction, were also determined. For comparison, eugenol was also tested. The results of this work could contribute to the development of vehicles with antioxidant potential estimated after 24 h of conducting the experiment, which indicates long-term protection against reactive oxygen species (ROS) in the deeper layers of the skin. The waste water from the clove buds steam distillation -contains several valuable biologically active compounds, and its use is environmentally friendly. We observed that gel vehicles were the best enhancer of skin permeation for both eugenol and its derivative. In most cases, -similar cumulative masses of eugenol and its ester were found in the acceptor fluid. The accumulation of EDChA was higher for cream vehicles in relation to the parent eugenol when applied onto the skin. The greatest amounts of eugenol were accumulated in the skin when these compounds were used in gel vehicles.

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