Deformable liposomes as enhancer of caffeine penetration through human skin in a Franz diffusion cell test

Abstract

ObjectiveThe permeation of hydrophilic molecules through the skin is still a challenge due to the barrier posed by stratum corneum, the outermost layer of the skin. Liposomes have frequently been used as carriers for different types of drugs and may also function as permeation enhancers. Propylene glycol has also been used as an edge activator in liposomes to increase the permeation. The aim of this work was to prepare liposomes containing an edge activator and loaded with caffeine to evaluate the potential of caffeine reaching the deeper layers in the skin.MethodsThe formulations were prepared by a top‐down process using high‐pressure homogenization at 200 00 psi for 10 min. They were characterized by size, polydispersity index (PI), zeta potential (ZP), pH, caffeine content and encapsulation efficiency (EE%) on preparation (time zero) and after 30 days. Cytotoxicity of blank and loaded liposomes was assessed by MTT proliferation assay with a normal keratinocyte cell line (HaCaT). In vitro permeation tests were performed with human skin in Franz cells over 24 h, and caffeine concentration was determined in the skin surface, stratum corneum, dermo‐epidermal fraction and receptor medium by HPLC.ResultsThe caffeine liposomes with (DL‐Caf) or without propylene glycol (CL‐Caf) showed, respectively, mean size 94.5 and 95.4 nm, PI 0.48 and 0.42, ZP + 1.3 and + 18.1 mV and caffeine content of 78.57 and 80.13%. IC50 values of caffeine in DL‐Caf (3.59 v/v %) and CL‐Caf (3.65 v/v %) were not significantly different from conventional blank liposome (3.27 v/v %). The DL‐Caf formulation presented the best capability to enhance the caffeine permeation through the skin, resulting 1.94‐folds higher than caffeine solution. Furthermore, the caffeine flux from DL‐Caf was 1.56‐ and 3.05‐folds higher than caffeine solution and CL‐Caf, respectively. On the other hand, CL‐Caf showed the lowest caffeine penetration revealing the importance of edge activator to aid hydrophilic drug penetration to all skin layers.ConclusionThe DL‐Caf formulation tested was able to improve the permeation of caffeine through the stratum corneum and dermo‐epidermal layers, suggesting that this delivery system may be effective for deep skin delivery of hydrophilic drugs.

The Impact of Improving Dermal Permeation on the Efficacy and Targeting of Liposome Nanoparticles as a Potential Treatment for Breast Cancer

“…These findings were agreed with Abdulbaqi, I.M., et al [11]. Cholesterol is a stiff molecule that improves the stability and rigidity of the lipid bilayer [8,33,36,37]. According to preliminary trials, increasing the cholesterol concentration produced stable deformable liposomal vesicles with a high % EE.…”

“…For small-scale deformable liposome production in a research laboratory, one of the simplest methods is thin film hydration [9,11]. Based on data collected from literature reviews, altering the phospholipid, cholesterol and PG concentrations are critical for deformable liposomes preparation [8,10,33]. Preliminary experiments were carried out, according to literature reviews, to determine the independent variable concentration ranges required for this study [8,10,33].…”

“…Based on data collected from literature reviews, altering the phospholipid, cholesterol and PG concentrations are critical for deformable liposomes preparation [8,10,33]. Preliminary experiments were carried out, according to literature reviews, to determine the independent variable concentration ranges required for this study [8,10,33]. Phospholipids contribute to the formation of lipid bilayers [9,34,35].…”

Determination of SLES in Personal Care Products by Colloid Titration with Light Reflection Measurements

“…The cationic polymer polyquaternium-10 is listed among the minor components. Cationic polymers are used in hair care products to improve the adsorption of active components on the hair surface [ 20 , 21 ]. Probably, polyquaternium is merely the component that forms the milky turbidity.…”

“…In general, hydrophobic interaction and secondary aggregation increase with the increase of the hydrophobic chain length in the surfactant molecule [ 19 ]. The self-association of polyDADMAC with anionic molecules is used to tune the adsorption of active cosmetic components on hair and skin surfaces [ 3 , 15 , 20 , 21 ].…”