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Assessment of urinary cotinine as a marker of nicotine absorption from tobacco leaves: a study on tobacco farmers in Malaysia

Onuki M, Yokoyama K, Kimura K, Sato H, Nordin RB, Naing L, et al.

J Occup Health, 2003 May;45(3):140-5.
PMID: 14646288

To assess dermal absorption of nicotine from tobacco leaves in relation to Green Tobacco Sickness (GTS), urinary cotinine concentrations were measured in 80 male tobacco-growing farmers and in 40 healthy males (controls) who did not handle wet tobacco leaves in Kelantan, Malaysia. Among non-smokers, urinary cotinine levels in farmers were significantly higher than those of controls; farmers with urinary cotinine of 50 ng/ml/m2 or above showed eye symptoms more frequently than those below this level (p<0.05). Farmers who did not wear protective equipment had subjective symptoms more frequently than those who used the equipment (p<0.05); some of these symptoms were seen more frequently in organophosphate (Tamaron) users than in non-users. As tobacco farmers evidence a risk of nicotine poisoning from tobacco leaves, assessment including GTS together with effects of pesticides will be necessary.

Matched MeSH terms: Skin Absorption
Mercury contamination in facial skin lightening creams and its health risks to user

Ho YB, Abdullah NH, Hamsan H, Tan ESS

Regul Toxicol Pharmacol, 2017 Aug;88:72-76.
PMID: 28554823 DOI: 10.1016/j.yrtph.2017.05.018

This study aims to determine concentrations of mercury in facial skin lightening cream according to different price categories (category I: skin lightening creams were determined during a preliminary market survey. Thereafter, twenty samples were purchased from various locations such as cosmetic stalls, beauty shops, pharmacies and street vendors based on their stratified price categories. Samples were extracted using microwave digester and analyzed using cold vapor atomic absorption spectrometry (CV-AAS). Non-carcinogenic chronic health risks for application of facial skin lightening cream were calculated using Dermal Absorption Dose (DAD) and Hazard Quotient (HQ). Concentrations of mercury in samples were less than the United States Food and Drug Administration (USFDA) permitted trace levels (<1 ppm) except for one sample from category III which was manufactured in China. Concentrations of mercury in facial skin lightening creams ranged from not detected to 1.13 mg kg-1. There was no significant association between concentrations of mercury with price categories (p = 0.12). There was no significant non-carcinogenic health risk due to daily application of the facial skin lightening creams based on assumption of 30 years exposure period (HQ

Matched MeSH terms: Skin Absorption
Fulltext Thermodynamic stability, in-vitro permeability, and in-silico molecular modeling of the optimal Elaeis guineensis leaves extract water-in-oil nanoemulsion

Romes NB, Abdul Wahab R, Abdul Hamid M, Oyewusi HA, Huda N, Kobun R

Sci Rep, 2021 10 21;11(1):20851.
PMID: 34675286 DOI: 10.1038/s41598-021-00409-0

Nanoemulsion is a delivery system used to enhance bioavailability of plant-based compounds across the stratum corneum. Elaeis guineensis leaves are rich source of polyphenolic antioxidants, viz. gallic acid and catechin. The optimal E. guineensis leaves extract water-in-oil nanoemulsion was stable against coalescence, but it was under significant influence of Ostwald ripening over 90 days at 25 °C. The in-vitro permeability revealed a controlled and sustained release of the total phenolic compounds (TPC) of EgLE with a cumulative amount of 1935.0 ± 45.7 µgcm-2 after 8 h. The steady-state flux and permeation coefficient values were 241.9 ± 5.7 µgcm-2 h-1 and 1.15 ± 0.03 cm.h-1, respectively. The kinetic release mechanism for TPC of EgLE was best described by the Korsmeyer-Peppas model due to the highest linearity of R2 = 0.9961, indicating super case II transport mechanism. The in-silico molecular modelling predicted that the aquaporin-3 protein in the stratum corneum bonded preferably to catechin over gallic acid through hydrogen bonds due to the lowest binding energies of - 57.514 kcal/mol and - 8.553 kcal/mol, respectively. Thus, the in-silico study further verified that catechin could improve skin hydration. Therefore, the optimal nanoemulsion could be used topically as moisturizer to enhance skin hydration based on the in-silico prediction.

Matched MeSH terms: Skin Absorption
The relevance of polymeric synthetic membranes in topical formulation assessment and drug diffusion study

Ng SF, Rouse JJ, Sanderson FD, Eccleston GM

Arch Pharm Res, 2012 Mar;35(4):579-93.
PMID: 22553050 DOI: 10.1007/s12272-012-0401-7

Synthetic membranes are composed of thin sheets of polymeric macromolecules that can control the passage of components through them. Generally, synthetic membranes used in drug diffusion studies have one of two functions: skin simulation or quality control. Synthetic membranes for skin simulation, such as the silicone-based membranes polydimethylsiloxane and Carbosil, are generally hydrophobic and rate limiting, imitating the stratum corneum. In contrast, synthetic membranes for quality control, such as cellulose esters and polysulfone, are required to act as a support rather than a barrier. These synthetic membranes also often contain pores; hence, they are called porous membranes. The significance of Franz diffusion studies and synthetic membranes in quality control studies involves an understanding of the fundamentals of synthetic membranes. This article provides a general overview of synthetic membranes, including a brief background of the history and the common applications of synthetic membranes. This review then explores the types of synthetic membranes, the transport mechanisms across them, and their relevance in choosing a synthetic membrane in Franz diffusion cell studies for formulation assessment purposes.

Matched MeSH terms: Skin Absorption
Formulation of diclofenac for dermal delivery

Goh CF, Lane ME

Int J Pharm, 2014 Oct 1;473(1-2):607-16.
PMID: 25091375 DOI: 10.1016/j.ijpharm.2014.07.052

Diclofenac (DF) was first synthesized in the 1960's and is currently available as ophthalmic, oral, parenteral, rectal and skin preparations. This review focuses on the administration of DF to the skin. As a member of the non-steroidal anti-inflammatory (NSAID) group of drugs the primary indications of DF are for the management of inflammation and pain but it is also used to treat actinic keratosis. The specific aims of this paper are to: (i) provide an overview of the pharmacokinetics and metabolism of DF following oral and topical administration; (ii) examine critically the various formulation approaches which have been investigated to enhance dermal delivery of DF; and (iii) identify new formulation strategies for enhanced DF skin penetration.

Matched MeSH terms: Skin Absorption
Reproducibility of laser Doppler fluximetry and the process of iontophoresis in assessing microvascular endothelial function using low current strength

Al-Tahami BA, Yvonne-Tee GB, Halim AS, Ismail AA, Rasool AH

Methods Find Exp Clin Pharmacol, 2010 Apr;32(3):181-5.
PMID: 20448860 DOI: 10.1358/mf.2010.32.3.1423887

Iontophoresis of acetylcholine (ACh) and sodium nitroprusside (SNP) combined with laser Doppler fluximetry (LDF) is a tool used to determine microvascular endothelial function. Our aim was to study the reproducibility of different parameters of this technique using iontophoresis with low current strength on the forearm skin of healthy subjects. Baseline skin perfusion was done before application of five current pulses with 1 min of current-free interval. Current strength of 0.007 mA, current density of 0.01 mA/cm(2) and charge density of 6 mC/cm(2) were used, along with 1% ACh and 1% SNP. The absolute maximum change in perfusion (max), percent change in perfusion (% change), peak change in perfusion (peak) and area under the curve during iontophoresis (AUC) at the anodal and cathodal leads were recorded. Measurements were performed in three sessions for 2 days. The coefficient of variation (CV) was calculated for each parameter. Among the parameters studied, maximum change in perfusion and peak flux were the most reproducible parameters.

Matched MeSH terms: Skin Absorption
Probing the effects of fish oil on the delivery and inflammation-inducing potential of imiquimod

Rehman K, Aluwi MF, Rullah K, Wai LK, Mohd Amin MC, Zulfakar MH

Int J Pharm, 2015 Jul 25;490(1-2):131-41.
PMID: 26003416 DOI: 10.1016/j.ijpharm.2015.05.045

Imiquimod is a chemotherapeutic agent for many skin-associated diseases, but it has also been associated with inflammatory side effects. The aim of this study was to prevent the inflammatory effect of commercial imiquimod (Aldara(®)) by controlled release of imiquimod through a hydrogel/oleogel colloidal mixture (CA bigel) containing fish oil as an anti-inflammatory agent. Imiquimod permeability from Aldara® cream and bigel through mice skin was evaluated, and the drug content residing in the skin via the tape stripping technique was quantified. The fish oil fatty acid content in skin along with its lipophilic environment was also determined. An inflammation study was conducted using animal models, and Aldara(®) cream was found to potentially cause psoriasis-like inflammation, which could be owing to prolonged application and excessive drug permeation. Controlled release of imiquimod along with fish oil through CA bigel may have caused reduced imiquimod inflammation. NMR studies and computerized molecular modeling were also conducted to observe whether the fish oil and imiquimod formed a complex that was responsible for improving imiquimod transport and reducing its side effects. NMR spectra showed dose-dependent chemical shifts and molecular modeling revealed π-σ interaction between EPA and imiquimod, which could help reduce imiquimod inflammation.

Matched MeSH terms: Skin Absorption
Fulltext Ethosomal nanocarriers: the impact of constituents and formulation techniques on ethosomal properties, in vivo studies, and clinical trials

Abdulbaqi IM, Darwis Y, Khan NA, Assi RA, Khan AA

Int J Nanomedicine, 2016;11:2279-304.
PMID: 27307730 DOI: 10.2147/IJN.S105016

Ethosomal systems are novel lipid vesicular carriers containing a relatively high percentage of ethanol. These nanocarriers are especially designed for the efficient delivery of therapeutic agents with different physicochemical properties into deep skin layers and across the skin. Ethosomes have undergone extensive research since they were invented in 1996; new compounds were added to their initial formula, which led to the production of new types of ethosomal systems. Different preparation techniques are used in the preparation of these novel carriers. For ease of application and stability, ethosomal dispersions are incorporated into gels, patches, and creams. Highly diverse in vivo models are used to evaluate their efficacy in dermal/transdermal delivery, in addition to clinical trials. This article provides a detailed review of the ethosomal systems and categorizes them on the basis of their constituents to classical ethosomes, binary ethosomes, and transethosomes. The differences among these systems are discussed from several perspectives, including the formulation, size, ζ-potential (zeta potential), entrapment efficiency, skin-permeation properties, and stability. This paper gives a detailed review on the effects of ethosomal system constituents, preparation methods, and their significant roles in determining the final properties of these nanocarriers. Furthermore, the novel pharmaceutical dosage forms of ethosomal gels, patches, and creams are highlighted. The article also provides detailed information regarding the in vivo studies and clinical trials conducted for the evaluation of these vesicular systems.

Matched MeSH terms: Skin Absorption
Transformation of Hydrophilic Drug into Oil-Miscible Ionic Liquids for Transdermal Drug Delivery

Md Moshikur R, Shimul IM, Uddin S, Wakabayashi R, Moniruzzaman M, Goto M

ACS Appl Mater Interfaces, 2022 Dec 21;14(50):55332-55341.
PMID: 36508194 DOI: 10.1021/acsami.2c15636

The transdermal delivery of hydrophilic drugs remains challenging owing to their poor ability to permeate the skin; formulation with oil media is difficult without adding chemical permeation enhancers or co-solvents. Herein, we synthesized 12 oil-miscible ionic liquid (IL) drugs comprising lidocaine-, imipramine-, and levamisole (Lev)-hydrochloride with fatty acid permeation enhancers, i.e., laurate, oleate, linoleate, and stearate as counterions. A set of in vitro and in vivo studies was performed to investigate the potency and deliverability of the transdermal drug formulations. All of the synthesized compounds were freely miscible with pharmaceutically acceptable solvents/agents (i.e., ethanol, N-methyl pyrrolidone, Tween 20, and isopropyl myristate (IPM)). In vitro permeation studies revealed that the oleate-based Lev formulation had 2.6-fold higher skin permeation capability than the Lev salts and also superior ability compared with the laurate-, linoleate-, and stearate-containing samples. Upon in vivo transdermal administration to mice, the peak plasma concentration, elimination half-life, and area under the plasma concentration curve values of Lev-IL were 4.6-, 2.9-, and 5.4-fold higher, respectively, than those of the Lev salt. Furthermore, in vitro skin irritation and in vivo histological studies have demonstrated that Lev-IL has excellent biocompatibility compared with a conventional ionic liquid-based carrier. The results indicate that oil-miscible IL-based drugs provide a simple and scalable strategy for the design of effective transdermal drug delivery systems.

Matched MeSH terms: Skin Absorption
Chitosan-based hydrogels: A comprehensive review of transdermal drug delivery

Tahir D, Ardiansyah A, Heryanto H, Noor EEM, Mohamed MA

Int J Biol Macromol, 2025 Apr;298:140010.
PMID: 39828168 DOI: 10.1016/j.ijbiomac.2025.140010

This article provides a comprehensive review of chitosan-based hydrogels for transdermal drug delivery. It covers various aspects including the chemical structure of chitosan and its derivatives, crosslinking agents, hydrogel morphology, and drug loading and release behaviors. The review draws on 16 studies sourced from Scopus, focusing on how the composition and structure of hydrogels influence drug release. The chemical structure of chitosan and its derivatives, such as chitosan hydrochloride and quaternary ammonium chitosan, plays a crucial role in determining the mechanical properties and stability of hydrogels. Crosslinking agents, both chemical and physical, affect the hydrogel's strength and transparency as well as its drug release profile. Hydrogel morphology, including its porosity, significantly impacts drug loading capacity and release behavior. Hydrogel-based microneedles show potential in overcoming the limitations of traditional drug administration methods by enhancing skin penetration and drug loading efficiency. Additionally, factors such as swelling ratio, drug loading efficiency, and release behavior are influenced by crosslinking methods, material composition, and environmental conditions. This article concludes that the design and modification of chitosan-based hydrogels can optimize transdermal drug delivery by improving drug release profiles and stability.

Matched MeSH terms: Skin Absorption
Effect of non-phospholipid-based cationic and phospholipid-based anionic nanosized emulsions on skin retention and anti-inflammatory activity of celecoxib

Tamilvanan S, Baskar R

Pharm Dev Technol, 2013 Jul-Aug;18(4):761-71.
PMID: 23668371 DOI: 10.3109/10837450.2011.586038

Celecoxib (CXB, 0.2 g)-loaded anionic and cationic nanosized emulsions were prepared by a well-established combined emulsification method.

Matched MeSH terms: Skin Absorption*
Dexibuprofen loaded into nanoemulsion based gel for topical application - In vitro characterization and in vivo anti-inflammatory evaluation

Munir R, Khan IU, Kamal Y, Asghar S, Irfan M, Alshammari A, et al.

Colloids Surf B Biointerfaces, 2025 Mar;247:114407.
PMID: 39616935 DOI: 10.1016/j.colsurfb.2024.114407

Arthritic disease is one of the most common diseases in adults and a leading cause of joint degeneration. Dexibuprofen (DEX) is routinely used for the treatment of rheumatoid arthritis, acute postoperative pain, primary dysmenorrheal, and in lower back pain. However, it is poorly water soluble with compromised bioavailability, and hence has limited therapeutic activity. In order to overcome these issues, we studied the formulation and characterization of nanoemulsion based system i.e nanoemulgel of DEX. This study aimed to prepare topical nanoemulgel containing 2 % DEX and solubility-enhanced DEX via ternary inclusion complexation (DEX-SE-T) and to compare it with commercially available 5 % Ibuprofen gel as there is no topical formulation of DEX is available in the market currently. A pseudoternary phase diagram was constructed using the spontaneous water titration method. Blank and drug-loaded nanoemulgel were prepared using a high-speed homogenization method. All the formulations were evaluated in terms of particle size, pH, conductivity, viscosity, zeta potential, and ex vivo drug permeation. DEX loaded nanoemulgel yield enhanced in vitro skin permeation than the commercially available 5 % ibuprofen gel. The optimized nanoemulgel formulation (DEX-SE-T) was tested in in vivo anti-inflammatory models including cotton pellets-induced abdominal granuloma (chronic inflammation) and carrageenan-induced paw edema (acute inflammation). DEX-SE-T loaded nanoemulgel has improved in vivo anti-inflammatory activity as compared to ibuprofen gel. DEX-SE-T could be a promising option for effective topical treatment of inflammatory conditions.

Matched MeSH terms: Skin Absorption/drug effects
Palm Olein Emulsion: a Novel Vehicle for Topical Drug Delivery of Betamethasone 17-Valerate

Ahmad K, Win T, Jaffri JM, Edueng K, Taher M

AAPS PharmSciTech, 2018 Jan;19(1):371-383.
PMID: 28744617 DOI: 10.1208/s12249-017-0843-9

This study aims to investigate the use of palm olein as the oil phase for betamethasone 17-valerate (BV) emulsions. The physicochemical properties of the formulations were characterized. In vitro drug release study was performed with the Hanson Vertical Diffusion Cell System; the samples were quantified with HPLC and the results were compared with commercial products. Optimized emulsion formulations were subjected to stability studies for 3 months at temperatures of 4, 25, and 40°C; the betamethasone 17-valerate content was analyzed using HPLC. The formulations produced mean particle size of 2-4 μm, viscosities of 50-250 mPa.s, and zeta potential between -45 and -68 mV. The rheological analyses showed that the emulsions exhibited pseudoplastic and viscoelastic behavior. The in vitro release of BV from palm olein emulsion through cellulose acetate was 4.5 times higher than that of commercial products and more BV molecules deposited in rat skin. Less than 4% of the drug was degraded in the formulations during the 3-month period when they were subjected to the three different temperatures. These findings indicate that palm olein-in-water emulsion can be an alternative vehicle for topical drug delivery system with superior permeability.

Matched MeSH terms: Skin Absorption
Transdermal delivery of raloxifene HCl via ethosomal system: Formulation, advanced characterizations and pharmacokinetic evaluation

Mahmood S, Mandal UK, Chatterjee B

Int J Pharm, 2018 May 05;542(1-2):36-46.
PMID: 29501737 DOI: 10.1016/j.ijpharm.2018.02.044

Raloxifene HCl belongs to a class of selective estrogen receptor modulators (SERMs) which is used for the management of breast cancer. The major problem reported with raloxifene is its poor bioavailability which is only up to 2%. The main objective of the present work was to formulate raloxifene loaded ethosomal preparation for transdermal application and compare it with an oral formulation of the drug. Five ethosomal formulations with different concentrations of ethanol and a conventional liposomes formulation were prepared by rotary evaporation method. The prepared systems were characterised by high resolution transmission electron microscopy (HRTEM), force emission electron microscopy (FESEM), atomic force microscopy (AFM), X-ray diffraction (XRD) and 31P NMR study. All these advanced characterization study established that the ethosome formulation was well defined by its size, shape and its bilayer formation. Transdermal flux of the optimized ethosome formulation was 22.14 ± 0.83 µg/ml/cm2 which was 21 times higher when compared to the conventional liposomes. Confocal microscopy study revealed an enhanced permeation of coumarin-6 dye loaded ethosomes to much deeper layers of skin when compared with conventional liposomes. The gel was found to be pseudoplastic with elastic behaviour. In-vivo studies on rats showed a higher bioavailability of RXL (157% times) for ethosomal formulation when compared with the oral formulation. In conclusion, RXL loaded ethosomal formulation via transdermal route showed superior drug delivery properties as compared to oral formulation.

Matched MeSH terms: Skin Absorption
Coenzyme Q10-Loaded Fish Oil-Based Bigel System: Probing the Delivery Across Porcine Skin and Possible Interaction with Fish Oil Fatty Acids

Zulfakar MH, Chan LM, Rehman K, Wai LK, Heard CM

AAPS PharmSciTech, 2018 Apr;19(3):1116-1123.
PMID: 29181705 DOI: 10.1208/s12249-017-0923-x

Coenzyme Q10 (CoQ10) is a vitamin-like oil-soluble molecule that has anti-oxidant and anti-ageing effects. To determine the most optimal CoQ10 delivery vehicle, CoQ10 was solubilised in both water and fish oil, and formulated into hydrogel, oleogel and bigel. Permeability of CoQ10 from each formulation across porcine ear skin was then evaluated. Furthermore, the effects of the omega-3 fatty eicosapentaenoic (EPA) and docosahexaenoic (DHA) acids from fish oil on skin permeation were investigated by means of nuclear magnetic resonance (NMR) and computerised molecular modelling docking experiments. The highest drug permeation was achieved with the bigel formulation that proved to be the most effective vehicle in delivering CoQ10 across the skin membrane due to a combination of its adhesive, viscous and lipophilic properties. Furthermore, the interactions between CoQ10 and fatty acids revealed by NMR and molecular modelling experiments likely accounted for skin permeability of CoQ10. NMR data showed dose-dependent changes in proton chemical shifts in EPA and DHA. Molecular modelling revealed complex formation and large binding energies between fatty acids and CoQ10. This study advances the knowledge about bigels as drug delivery vehicles and highlights the use of NMR and molecular docking studies for the prediction of the influence of drug-excipient relationships at the molecular level.

Matched MeSH terms: Skin Absorption
Influence of omega fatty acids on skin permeation of a coenzyme Q10 nanoemulsion cream formulation: characterization, in silico and ex vivo determination

Tou KAS, Rehman K, Ishak WMW, Zulfakar MH

Drug Dev Ind Pharm, 2019 Sep;45(9):1451-1458.
PMID: 31216907 DOI: 10.1080/03639045.2019.1628042

Objective: The aim of this study was to develop a coenzyme Q10 nanoemulsion cream, characterize and to determine the influence of omega fatty acids on the delivery of coenzyme Q10 across model skin membrane via ex vivo and in silico techniques. Methods: Coenzyme Q10 nanoemulsion creams were prepared using natural edible oils such as linseed, evening primrose, and olive oil. Their mechanical features and ability to deliver CoQ10 across rat skin were characterized. Computational docking analysis was performed for in silico evaluation of CoQ10 and omega fatty acid interactions. Results: Linseed, evening primrose, and olive oils each produced nano-sized emulsion creams (343.93-409.86 nm) and exhibited excellent rheological features. The computerized docking studies showed favorable interactions between CoQ10 and omega fatty acids that could improve skin permeation. The three edible-oil nanoemulsion creams displayed higher ex vivo skin permeation and drug flux compared to the liquid-paraffin control cream. The linseed oil formulation displayed the highest skin permeation (3.97 ± 0.91 mg/cm2) and drug flux (0.19 ± 0.05 mg/cm2/h). Conclusion: CoQ10 loaded-linseed oil nanoemulsion cream displayed the highest skin permeation. The highest permeation showed by linseed oil nanoemulsion cream may be due to the presence of omega-3, -6, and -9 fatty acids which might serve as permeation enhancers. This indicated that the edible oil nanoemulsion creams have potential as drug vehicles that enhance CoQ10 delivery across skin.

Matched MeSH terms: Skin Absorption
Biocompatible Ionic Liquid-Mediated Micelles for Enhanced Transdermal Delivery of Paclitaxel

Ali MK, Moshikur RM, Wakabayashi R, Moniruzzaman M, Goto M

ACS Appl Mater Interfaces, 2021 May 05;13(17):19745-19755.
PMID: 33891816 DOI: 10.1021/acsami.1c03111

Chemotherapeutic cytotoxic agents such as paclitaxel (PTX) are considered essential for the treatment of various cancers. However, PTX injection is associated with severe systemic side effects and high rates of patient noncompliance. Micelle formulations (MFs) are nano-drug delivery systems that offer a solution to these problems. Herein, we report an advantageous carrier for the transdermal delivery of PTX comprising a new MF that consists of two biocompatible surfactants: cholinium oleate ([Cho][Ole]), which is a surface-active ionic liquid (SAIL), and sorbitan monolaurate (Span-20). A solubility assessment confirmed that PTX was readily solubilized in the SAIL-based micelles via multipoint hydrogen bonding and cation-π and π-π interactions between PTX and SAIL[Cho][Ole]. Dynamic light scattering (DLS) and transmission electron microscopy revealed that in the presence of PTX, the MF formed spherical PTX-loaded micelles that were well-distributed in the range 8.7-25.3 nm. According to DLS, the sizes and size distributions of the micelle droplets did not change significantly over the entire storage period, attesting to their physical stability. In vitro transdermal assessments using a Franz diffusion cell revealed that the MF absorbed PTX 4 times more effectively than a Tween 80-based formulation and 6 times more effectively than an ethanol-based formulation. In vitro and in vivo skin irritation tests revealed that the new carrier had a negligible toxicity profile compared with a conventional ionic liquid-based carrier. Based on these findings, we believe that the SAIL[Cho][Ole]-based MF has potential as a biocompatible nanocarrier for the effective transdermal delivery of poorly soluble chemotherapeutics such as PTX.

Matched MeSH terms: Skin Absorption
Cubosome-based skin delivery: from topical to transdermal applications

Gunawan M, Efendi A, Ramadon D, Liew CV, Chutoprapat R

Expert Opin Drug Deliv, 2026 Nov;23(11):2059-2087.
PMID: 42779272 DOI: 10.1080/17425247.2026.2739504

INTRODUCTION: Skin delivery provides an alternative drug administration, although its effectiveness is limited by the stratum corneum barrier. Cubosomes, as third-generation lipid nanoparticles with bicontinuous cubic liquid crystalline structures, have emerged as promising nanocarriers that enhance skin penetration, sustain drug release, improve bioavailability, and minimize toxicity.
AREAS COVERED: This review discusses the biopharmaceutical mechanisms of cubosome-mediated skin delivery, including bioadhesion, stratum corneum lipid fluidization, controlled release, enhanced cellular uptake, and improved bioavailability. Literature from 2006-2026 was collected from Scopus, PubMed, and patent databases, covering localized applications such as dermatological disorders, wound healing, fungal infections, alopecia, inflammatory skin diseases, and oncology, as well as systemic therapies including rheumatoid arthritis, gout, diabetes mellitus, and hormone replacement therapy. Recent advances, including microneedle integration, thermosensitive hydrogels, stimuli-responsive systems, and surface-engineered cubosomes, are also highlighted.
EXPERT OPINION: Cubosomes represent a promising platform for advanced skin delivery. Optimal performance depends on the therapeutic goal, with systemic delivery requiring enhanced permeation and sustained absorption, whereas localized therapy prioritizes intradermal retention and tissue depot formation with minimal systemic exposure. Despite strong preclinical evidence, further studies on long-term safety, manufacturing standardization, and clinical validation are essential for successful clinical translation and commercialization of cubosome-based skin delivery.

Matched MeSH terms: Skin Absorption
Chitosan-Carboxymethyl-5-Fluorouracil-Folate Conjugate Particles: Microwave Modulated Uptake by Skin and Melanoma Cells

Nawaz A, Wong TW

J Invest Dermatol, 2018 11;138(11):2412-2422.
PMID: 29857069 DOI: 10.1016/j.jid.2018.04.037

5-Fluorouracil delivery profiles in the form of chitosan-folate submicron particles through skin and melanoma cells in vitro were examined using microwaves as the penetration enhancer. The in vivo pharmacokinetic profile of 5-fluorouracil was also determined. Chitosan-carboxymethyl-5-fluorouracil-folate conjugate was synthesized and processed into submicron particles by spray-drying technique. The size, zeta potential, morphology, drug content, and drug release, as well as skin permeation and retention, pharmacokinetics, in vitro SKMEL-28 melanoma cell line cytotoxicity, and intracellular trafficking profiles of drug/particles, were examined as a function of skin/melanoma cell treatment by microwaves at 2,450 MHz for 5 + 5 minutes. The level of skin drug/particle retention in vitro and in vivo increased in skin treated by microwaves. This was facilitated by the drug conjugating to chitosan and microwaves fluidizing both the protein and lipid domains of epidermis and dermis. The uptake of chitosan-folate particles by melanoma cells was mediated via lipid raft route. It was promoted by microwaves, which fluidized the lipid and protein regimes of the cell membrane, and this increased drug cytotoxicity. In vivo pharmacokinetic study indicated skin treatment by microwave-enhanced drug retention but not permeation. The combination of microwaves and submicron particles synergized skin drug retention and intracellular drug delivery.

Matched MeSH terms: Skin Absorption
Fulltext Formulation and in vitro release evaluation of newly synthesized palm kernel oil esters-based nanoemulsion delivery system for 30% ethanolic dried extract derived from local Phyllanthus urinaria for skin antiaging

Mahdi ES, Noor AM, Sakeena MH, Abdullah GZ, Abdulkarim MF, Sattar MA

Int J Nanomedicine, 2011;6:2499-512.
PMID: 22072884 DOI: 10.2147/IJN.S22337

BACKGROUND: Recently there has been a remarkable surge of interest about natural products and their applications in the cosmetic industry. Topical delivery of antioxidants from natural sources is one of the approaches used to reverse signs of skin aging. The aim of this research was to develop a nanoemulsion cream for topical delivery of 30% ethanolic extract derived from local Phyllanthus urinaria (P. urinaria) for skin antiaging.
METHODS: Palm kernel oil esters (PKOEs)-based nanoemulsions were loaded with P. urinaria extract using a spontaneous method and characterized with respect to particle size, zeta potential, and rheological properties. The release profile of the extract was evaluated using in vitro Franz diffusion cells from an artificial membrane and the antioxidant activity of the extract released was evaluated using the 2, 2-diphenyl-1-picrylhydrazyl (DPPH) method.
RESULTS: Formulation F12 consisted of wt/wt, 0.05% P. urinaria extract, 1% cetyl alcohol, 0.5% glyceryl monostearate, 12% PKOEs, and 27% Tween 80/Span 80 (9/1) with a hydrophilic lipophilic balance of 13.9, and a 59.5% phosphate buffer system at pH 7.4. Formulation F36 was comprised of 0.05% P. urinaria extract, 1% cetyl alcohol, 1% glyceryl monostearate, 14% PKOEs, 28% Tween 80/Span 80 (9/1) with a hydrophilic lipophilic balance of 13.9, and 56% phosphate buffer system at pH 7.4 with shear thinning and thixotropy. The droplet size of F12 and F36 was 30.74 nm and 35.71 nm, respectively, and their nanosizes were confirmed by transmission electron microscopy images. Thereafter, 51.30% and 51.02% of the loaded extract was released from F12 and F36 through an artificial cellulose membrane, scavenging 29.89% and 30.05% of DPPH radical activity, respectively.
CONCLUSION: The P. urinaria extract was successfully incorporated into a PKOEs-based nanoemulsion delivery system. In vitro release of the extract from the formulations showed DPPH radical scavenging activity. These formulations can neutralize reactive oxygen species and counteract oxidative injury induced by ultraviolet radiation and thereby ameliorate skin aging.

Matched MeSH terms: Skin Absorption

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