A Novel Natural Penetration Enhancer for Transdermal Drug Delivery: In Vitro/In Vivo Evaluation and Penetration Enhancement Mechanism

Pharmaceutics, Journal Year: 2025, Volume and Issue: 17(2), P. 254 - 254

Published: Feb. 14, 2025

Objectives: This study aimed to identify and develop a novel, safe, effective transdermal penetration enhancer derived from the leaves of Perilla frutescens (L.) Britt, explore underlying mechanisms its enhancement effects. Methods: To evaluate safety profile enhancer, both skin irritation tests histopathological analyses were conducted. The capabilities assessed in vitro using five model drugs. Furthermore, gain insights into mechanism this novel range analytical methods used, including spectroscopic technique, differential scanning calorimetry, micro-optical techniques, molecular docking simulations. Results: essential oil contained 93.70% perilla ketone (PEK), which exhibited superior that azone. PEK significantly increased cumulative permeation all drugs (p < 0.05). most obvious impact on puerarin penetration, with quantitative ratios 2.96 ± 0.07 3.39 0.21 at concentrations 3% 5% (w/v), respectively. A strong correlation between effect physicochemical properties was observed. Mechanistic studies revealed facilitates drug distribution solution phase stratum corneum (SC). Conclusions: PEK, seldom discussed former studies, observed show extensive effects by inducing conformational changes SC lipids disrupting tightly ordered bilayer arrangement lipids. These findings highlight potential as promising safe natural enhancer.

Language: Английский

Phospholipid-Based Vesicular Systems as Carriers for the Delivery of Active Cosmeceutical Ingredients

International Journal of Molecular Sciences, Journal Year: 2025, Volume and Issue: 26(6), P. 2484 - 2484

Published: March 11, 2025

Cosmeceuticals are cosmetic products containing biologically active ingredients claiming to have drug-like benefits. In recent years, there has been a growing global demand for cosmeceuticals focusing on visible improvement of skin appearance and health. However, modern consumers increasingly more concerned about the performance clinical efficacy formulations. One main disadvantages cosmeceutical preparations is poor transdermal delivery included in formulation. response this challenge, many phospholipid-based nanovesicular systems developed tested years increase penetration molecules. This review provides comprehensive overview current knowledge research development liposomal encapsulation used as system skincare products.

Language: Английский

Enhancing collagen based nanoemulgel for effective topical delivery of Aceclofenac and Citronellol oil: Formulation, optimization, in-vitro evaluation, and in-vivo osteoarthritis study with a focus on HMGB-1/RAGE/NF-κB pathway, Klotho, and miR-499a

Drug Delivery and Translational Research, Journal Year: 2024, Volume and Issue: 14(11), P. 3250 - 3268

Published: March 19, 2024

Abstract The majority of conventional osteoarthritis (OA) treatments are based on molecular adjustment certain signaling pathways associated with pathogenesis, however there is a significant need to search for more effective and safe treatments. This study centers around formulating Aceclofenac (ACF) high bioavailability in combination Citronellol oil collagen. optimal concentrations oil/D-Limonene oil, Tween 80, Transcutol HP were determined using pseudoternary phase diagram. formulated nanoemulsions studied thermophysical stability. Thermodynamically stable formula analyzed droplet size, zeta potential, in-vitro permeation. Then, collagen nanoemulsion prepared capitalize its efficacy reducing side effects characterized nano size properties. Formulae F10 F10C chosen as optimum nanosize formula. Hense, they nanoemulgel dosage form. formulae F10NEG1 F10CNEG1 showed reasonable viscosity spreadability, complete drug release after 4 h. These further In vivo anti-OA study. Collagen ACF/citronellol emugel able modulate HMGB-1/RAGE/NF-κB pathway, mitigating the production inflammatory cytokine TNF-α. They also Klotho miR-499, serum CTXII COMP, by cartilage destruction. Histological investigations validated efficacy, safety, superiority (F10CNEG1) over solo treated group (F10NEG1 blank). Hence, findings current work encourage use this promising combined treatment OA patients. Graphical abstract

Language: Английский