Penetration Of Active Ingredients Research Articles

Liposome-assisted penetration and antiaging effects of collagen in a 3D skin model.

Collagen is a major component of the extracellular matrix that supports the epidermal layers of the skin; thus, many strategies have been made to enhance the topical delivery of collagen for antiaging purposes. In addition, our previous study indicated that liposome can help the penetration of active ingredients into the skin. To produce stable collagen-encapsulated liposomes to improve the topical delivery of collagen. Collagen-encapsulated liposomes were fabricated using high-pressure homogenization method. The colloidal stability and adhesion ability were confirmed using dynamic light scattering, and spectrofluorophotometer, respectively. Keratinocyte differentiations of 3D skin before and after treatment with collagen-encapsulated liposomes were confirmed by real-time PCR. In comparison with native collagen, collagen-encapsulated liposomes enhanced collagen retention in artificial membranes by twofold, even after repeated washings with water. In addition, real-time PCR results indicated that 3D skin treated with collagen-encapsulated liposomes exhibited higher levels of collagen, keratin, and involucrin, even after ethanol treatment. Liposomes could serve as efficient delivery vehicles for collagen, thereby enhancing its antiaging effects.

Influence of Massage and Skin Hydration on Dermal Penetration Efficacy of Nile Red from Petroleum Jelly-An Unexpected Outcome.

The study aimed at comparing the influence of direct and indirect skin hydration as well as massage on the dermal penetration efficacy of active compounds. Nile red was used as a lipophilic drug surrogate and was incorporated into Vaseline (petroleum jelly). The formulation was applied with and without massage onto either dry skin or pre-hydrated, moist skin. It was expected that the occlusive properties of Vaseline in combination with massage and enhanced skin hydration would cause a superposition of penetration-enhancing effects, which should lead to a tremendous increase in the dermal penetration efficacy of the lipophilic drug surrogate. Results obtained were diametral to the expectations, and various reasons were identified for causing the effect observed. Firstly, it was found that Vaseline undergoes syneresis after topical application. The expulsed mineral oil forms a film on top of the skin, and parts of it penetrate into the skin. The lipophilic drug surrogate, which is dissolved in the mineral oil, enters the skin with the mineral oil, i.e., via a solvent drag mechanism. Secondly, it was found that massage squeezes the skin and causes the expulsion of water from deeper layers of the SC. The expulsed water can act as a water barrier that prevents the penetration of lipophilic compounds and promotes the penetration of hydrophilic compounds. Based on the data, it is concluded that dermal penetration is a complex process that cannot only be explained by Fick’s law. It is composed of at least three different mechanisms. The first mechanism is the penetration of active ingredients with their solvents into the skin (convection, solvent drag), the second mechanism is the penetration of the active ingredient via passive diffusion, and the third mechanism can involve local penetration phenomena, e.g., the formation of liquid menisci and particle-associated penetration enhancement, which occur upon the evaporation of water and/or other ingredients from the formulation on top of the skin.

Novel Rotational Combination Regimen of Skin Topicals Improves Facial Photoaging: Efficacy Demonstrated in Double-Blinded Clinical Trials and Laboratory Validation.

Topical antiaging products are often a first-line intervention to counter visible signs of facial photoaging, aiming for sustained cosmetic improvement. However, prolonged application of a single active topical compound was observed clinically to lead to a plateau effect in improving facial photoaging. In view of this, we set out to reduce this effect systematically using a multi-tiered approach with laboratory evidence and clinical trials. The objective of the study was to evaluate the effects of active topical ingredients applied either alone, in combination, or in a rotational manner on modulation of facial photoaging. The study methodology included in vitro, organotypic, and ex vivo skin explants; in vivo biopsy study; as well as clinical trials. We demonstrate for the first time that a pair of known antiaging ingredients applied rotationally, on human dermal fibroblasts, maximized pro-collagen I production. Indeed, rotational treatment with retinol and phytol/glycolic acid (PGA) resulted in better efficacy than application of each active ingredient alone as shown by explants and in vivo biopsy study, with penetration of active ingredients confirmed by Raman spectroscopy. Furthermore, two split-face, randomized, double-blinded clinical trials were conducted, one for 12 months to compare treated vs. untreated and the other for 6 months followed by a 2-month regression to compare treated vs. commercially marketed products. In both studies, rotational regimen showed superior results to its matching comparison as assessed by clinical grading and image analysis of crow's feet wrinkles. In conclusion, rotational regimen using retinol and PGA is effective in treating facial photoaging signs with long-lasting benefits.

LB730 Quantitative skin-penetration evaluation of active ingredients on in-vitro 3D skin model using confocal Raman spectroscopy

The penetration of active ingredients from topically applied skincare products impacts their efficacy. Many measurement methodologies have been devised to address how fast and how much ingredient molecules penetrate into skin. Here, we established an experimental and analytical method using confocal Raman spectroscopy and demonstrated a quantitative and spatiotemporal penetration profile of active ingredients into skin. We generated standard curves (Raman signal vs. concentration) for certain active ingredients, using agar gel skin phantom.

Effects of surfactants on foliar uptake of herbicides – a complex scenario

Surfactants are almost always present in herbicide treatment solutions with the aim to improve spray droplet retention on and penetration of active ingredients (a.i.s) into plant foliage. The effects of surfactants on the foliar uptake of herbicides are complex and only partially understood. The influence of a range of non-ionic polyoxyethylene surfactants on the uptake of two herbicides, glyphosate and 2,4-dichlorophenoxyacetic acid (2,4-D), was compared using three plant species, wheat, broad bean and common lambsquarters. Surfactants of higher ethylene oxide (EO) content provided greater uptake enhancement for glyphosate, whereas those of lower EO content were more beneficial for 2,4-D uptake. Among surfactants of the same EO content, those containing a C 13/C 15 linear alkane hydrophobe moiety appeared to be more efficient for promoting the uptake of both herbicides. When a suitable surfactant was used, glyphosate uptake into both bean and wheat foliage increased steadily with increasing surfactant concentration and reached a maximum at 0.5%. In the presence of a constant surfactant, higher percentage uptake of herbicide was obtained with higher a.i. concentrations for glyphosate, but with lower a.i. concentrations in the case of 2,4-D. In the presence of an organosilicone surfactant, the stomatal uptake of glyphosate varied with both surfactant concentration and plant species. The effect of non-silicone surfactants on the cuticular uptake of glyphosate also varied with plant species. It can be concluded that the effects of surfactants on foliar uptake of herbicides depend not only on their chemical structures (hydrophobe and hydrophile moieties) and concentration, but also on the physicochemical properties and concentration of a.i.s and the leaf surface character of the plant species.

Topical penetration of commercial salicylate esters and salts using human isolated skin and clinical microdialysis studies.

The penetration of active ingredients from topically applied anti-inflammatory pharmaceutical products into tissues below the skin is the basis of their therapeutic efficacy. There is still controversy as to whether these agents are capable of direct penetration by diffusion through the tissues or whether redistribution in the systemic circulation is responsible for their tissue deposition below the application site. The extent of direct penetration of salicylate from commercial ester and salt formulations into the dermal and subcutaneous tissue of human volunteers was determined using the technique of cutaneous microdialysis. We also examined differences in the extent of hydrolysis of the methylester of salicylate applied topically in human volunteers and in vitro skin diffusion cells using full-thickness skin and epidermal membranes. The present study showed that whilst significant levels of salicylate could be detected in the dermis and subcutaneous tissue of volunteers treated with the methylsalicylate formulation, negligible levels of salicylate were seen following application of the triethanolamine salicylate formulation. The tissue levels ofsalicylate from the methylsalicylate formulation were approx. 30-fold higher than the plasma concentrations. The absorption and tissue concentration profiles for the commercial methylsalicylate formulation are indicative of direct tissue penetration and not solely redistribution by the systemic blood supply.

The formulation of drug for ocular administration.

The different barriers that slow the penetration of active ingredients administered by the ocular route are described, and some novel dosage forms designed for this route are discussed. Both precorneal and corneal factors considerably restrict ocular penetration. The low bioavailability of classical ophthalmic dosage forms can be improved by several approaches, particularly by increasing the time the active ingredients remain in contact with the eye tissues. The new dosage forms are reviewed according to their type and their drug release mechanisms. The characteristics, advantages, and limitations of each are outlined. The potential of these dosage forms can be expected to enhance development. They offer prolonged effectiveness, reproducibility, fewer unwanted side effects, and improved tolerance.