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The giant mudskipper Periophthalmodon schlosseri facilitates active NH(4)(+) excretion by increasing acid excretion and decreasing NH(3) permeability in the skin

Ip YK, Randall DJ, Kok TK, Barzaghi C, Wright PA, Ballantyne JS, et al.

J Exp Biol, 2004 Feb;207(Pt 5):787-801.
PMID: 14747411

Periophthalmodon schlosseri is an amphibious and obligatory air-breathing teleost, which is extremely tolerant to environmental ammonia. It actively excretes NH(4)(+) in ammonia loading conditions. For such a mechanism to operate efficaciously the fish must be able to prevent back flux of NH(3). P. schlosseri could lower the pH of 50 volumes (w/v) of 50% seawater in an artificial burrow from pH 8.2 to pH 7.4 in 1 day, and established an ambient ammonia concentration of 10 mmol l(-1) in 8 days. It could alter the rate of titratable acid efflux in response to ambient pH. The rate of net acid efflux (H(+) excretion) in P. schlosseri was pH-dependent, increasing in the order pH 6.0<7.0<8.0<8.5. Net acid flux in neutral or alkaline pH conditions was partially inhibited by bafilomycin, indicating the possible involvement of a V-type H(+)-ATPase. P. schlosseri could also increase the rate of H(+) excretion in response to the presence of ammonia in a neutral (pH 7.0) external medium. Increased H(+) excretion in P. schlosseri occurred in the head region where active excretion of NH(4)(+) took place. This would result in high concentrations of H(+) in the boundary water layer and prevent the dissociation of NH(4)(+), thus preventing a back flux of NH(3) through the branchial epithelia. P. schlosseri probably developed such an 'environmental ammonia detoxification' capability because of its unique behavior of burrow building in the mudflats and living therein in a limited volume of water. In addition, the skin of P. schlosseri had low permeability to NH(3). Using an Ussing-type apparatus with 10 mmol l(-1) NH(4)Cl and a 1 unit pH gradient (pH 8.0 to 7.0), the skin supported only a very small flux of NH(3) (0.0095 micromol cm(-2) min(-1)). Cholesterol content (4.5 micromol g(-1)) in the skin was high, which suggests low membrane fluidity. Phosphatidylcholine, which has a stabilizing effect on membranes, constituted almost 50% of the skin phospholipids, with phosphatidyleserine and phsophatidylethanolamine contributing only 13% and 15%, respectively. More importantly, P. schlosseri increased the cholesterol level (to 5.5 micromol g(-1)) and altered the fatty acid composition (increased total saturated fatty acid content) in its skin lipid after exposure to ammonia (30 mmol l(-1) at pH 7.0) for 6 days. These changes might lead to an even lower permeability to NH(3) in the skin, and reduced back diffusion of the actively excreted NH(4)(+) as NH(3) or the net influx of exogenous NH(3), under such conditions.

Matched MeSH terms: Skin/metabolism
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/metabolism*
Hydrogel-gauze dressing for moderate-to-severe atopic dermatitis: development and efficacy study on atopic dermatitis-like skin lesions in NC/Nga mice

Ng SF, Lew PC, Sin YB

Drug Dev Ind Pharm, 2014 Nov;40(11):1538-46.
PMID: 24025072 DOI: 10.3109/03639045.2013.836214

Topical emollients are known to provide symptomatic relief for atopic dermatitis. In hospitals, wet-wrap therapy has been shown to benefit children with moderate-to-severe atopic dermatitis (AD), but the application of wet-wraps is tedious and time-consuming. Topical emollients have low residence time and often dry out easily. The aim of this work was to develop a hydrogel-gauze dressing that is not only easy to apply but also rehydrates and traps moisture to provide longer relief for AD patients. In this study, a prototype hydrogel-gauze dressing was developed with varying ratios of sodium carboxymethylcellulose (NaCMC) and propylene glycol. The hydrogel-gauze dressings were assessed based on the moisture vapor transmission rate, moisture absorption, mechanical properties and storage stability over three months. Then, the efficacy of the hydrogel-gauze dressing was compared to topical emollients using transgenic NC/Nga mice with AD-like lesions. The NaCMC hydrogel-gauze dressings significantly lowered transepidermal water loss, and the animals displayed a faster recovery, which indicates that hydrogel-gauze dressings can trap moisture more effectively and accelerate AD healing. Hence, we propose that hydrogel-gauze dressings can potentially become an alternative to wet-wrap therapy due to the ease of application and the higher efficacy compared to topical products.

Matched MeSH terms: Skin/metabolism
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/metabolism
Transdermal delivery of oxybutynin chloride proniosomal gels for the treatment of overactive bladder

Rajabalaya R, David SR, Chellian J, Xin Yun G, Chakravarthi S

Drug Deliv, 2016 Jun;23(5):1578-87.
PMID: 26634274 DOI: 10.3109/10717544.2015.1116027

CONTEXT: Overactive bladder (OAB) is a common problem and anticholinergic drugs are first-line therapy, but they have side effects.
OBJECTIVE: Development of oxybutynin chloride (OC) proniosomal gels and analyses of its efficacy for OAB treatment.
MATERIALS AND METHODS: Phase separation coacervation was used to prepare proniosomal gels using various non-ionic surfactants, lipids, soy lecithin and isopropyl alcohol. Gels were characterized with regard to entrapment efficiency (EE), vesicle size, surface morphology (using environmental scanning electron microscopy [E-SEM]), stability, attenuated total reflectance Fourier transform infrared (ATR-FTIR) spectroscopy, in vitro skin permeation, in vivo animal studies and histopathology.
RESULTS AND DISCUSSION: EE was 87-92%, vesicle size was 0.38-5.0 μm, and morphology showed some loosened pores in proniosomes after hydration. ATR-FTIR spectroscopy showed no significant shifts in peaks corresponding to OC and excipients. Most formulations exhibited >50% permeation but the cholesterol-containing formulations P3 (Span 20:Span 60 [1:1]) and P4 [Tween 20:Tween 80 (1:1)] had the highest percent cumulative permeation. P3 and P4 also showed faster recovery of cholinergic effects on salivary glands than oral formulations. P3 and P4 had pronounced therapeutic effects in reduction of urinary frequency and demonstrated improvements in bladder morphology (highly regenerative surface of the transitional epithelium).
CONCLUSION: These results suggest that OC could be incorporated into proniosomal gels for transdermal delivery in the treatment of OAB.

Matched MeSH terms: Skin/metabolism*
Permeation Studies of Captopril Transdermal Films Through Human Cadaver Skin

Nair RS, Nair S

Curr Drug Deliv, 2015;12(5):517-23.
PMID: 25675336

Mortality rate due to heart diseases increases dramatically with age. Captopril is an angiotensin converting enzyme inhibitor (ACE) used effectively for the management of hypertension. Due to short elimination half-life of captopril the oral dose is very high. Captopril is prone to oxidation and it has been reported that the oxidation rate of captopril in skin tissues is considerably low when compared to intestinal tissues. All these factors make captopril an ideal drug candidate for transdermal delivery. In this research work an effort was made to formulate transdermal films of captopril by utilizing polyvinylpyrrolidone (PVP) and polyvinyl alcohol (PVA) as film formers and polyethylene glycol 400 (PEG400) as a plasticizer. Dimethyl sulfoxide (DMSO) and dimethylformamide (DMF) were used as permeation enhancers. Physicochemical parameters of the films such as appearance, thickness, weight variation and drug content were evaluated. The invitro permeation studies were carried out through excised human cadaver skin using Franz diffusion cells. The in-vitro permeation studies demonstrated that the film (P4) having the polymer ratio (PVP:PVA = 80:20) with DMSO (10%) resulted a promising drug release of 79.58% at 24 hours with a flux of 70.0 µg/cm(2)/hr. No signs of erythema or oedema were observed on the rabbit skin as a result of skin irritation study by Draize test. Based on the stability report it was confirmed that the films were physically and chemically stable, hence the prepared films are very well suited for transdermal application.

Matched MeSH terms: Skin/metabolism*
Electrical, magnetic, photomechanical and cavitational waves to overcome skin barrier for transdermal drug delivery

Wong TW

J Control Release, 2014 Nov 10;193:257-69.
PMID: 24801250 DOI: 10.1016/j.jconrel.2014.04.045

Transdermal drug delivery is hindered by the barrier property of the stratum corneum. It limits the route to transport of drugs with a log octanol-water partition coefficient of 1 to 3, molecular weight of less than 500Da and melting point of less than 200°C. Active methods such as iontophoresis, electroporation, sonophoresis, magnetophoresis and laser techniques have been investigated for the past decades on their ability, mechanisms and limitations in modifying the skin microenvironment to promote drug diffusion and partition. Microwave, an electromagnetic wave characterized by frequencies range between 300MHz and 300GHz, has recently been reported as the potential skin permeation enhancer. Microwave has received a widespread application in food, engineering and medical sectors. Its potential use to facilitate transdermal drug transport is still in its infancy stage of evaluation. This review provides an overview and update on active methods utilizing electrical, magnetic, photomechanical and cavitational waves to overcome the skin barrier for transdermal drug administration with insights into mechanisms and future perspectives of the latest microwave technique described.

Matched MeSH terms: Skin/metabolism
Deposition of tocopherol and tocotrienol in the tissues of red hybrid tilapia, Oreochromis sp., fed vitamin E-free diets supplemented with different plant oils

Lee KS, Yuen KH, Ng WK

Fish Physiol Biochem, 2013 Dec;39(6):1457-71.
PMID: 23604920 DOI: 10.1007/s10695-013-9799-1

Vitamin E, a potent antioxidant consisting of four isomers each (α, β, γ, δ) of tocopherol (T) and tocotrienol (T3), is found naturally in plant oils at different concentrations. In this study, four semi-purified isonitrogenous and isolipidic (10 %) diets containing canola oil, cold-pressed soybean oil, wheat germ oil, or palm fatty acid distillates (PFAD) as the sole vitamin E source were fed to triplicate groups of red hybrid tilapia (Oreochromis sp.) fingerlings (14.82 ± 0.05 g) for 45 days. Vitamin E concentrations and composition were measured in the muscle, liver, skin, and adipose tissue. Deposition of α-T (53.4-93.1 % of total vitamin E) predominated over deposition of other isomers, except in the liver of fish fed the SBO diet, where α-T and γ-T deposition was in the ratio 40:60. T3 deposition (2.6-29.4 %) was only detected in tissues of fish fed the PFAD diet; adipose tissue was the major storage depot. Fish fed the SBO diet contained significantly more (P

Matched MeSH terms: Skin/metabolism
Lack of increased P15INK4B protein expression in basal cell carcinomas

Moad AI, Tan ML, Kaur G, Mabruk M

Asian Pac J Cancer Prev, 2012;13(12):6239-44.
PMID: 23464438

BACKGROUND: The basal cell carcinoma (BCC) is the most common non-melanoma skin cancer (NMSK). BCC might develop because of the faulty cell cycle arrest. P15INK4b is a tumor suppressor gene, involved in cell cycle arrest and inactivated in most human cancers. The role of p15INK4b protein expression in the genesis of BCC is as yet unknown. In a previous study we showed the absence of p15INK4b expression in the majority of tissue microarray cores of cutaneous squamous cell carcinoma (SCCs), another type of non-melanoma skin cancer, indicating that p15INK4b could possibly be involved in the pathogenesis of cutaneous SCC. The aim of this study was to investigate p15INK4b protein expression in BCCs.
MATERIALS AND METHOD: Protein expression of p15INK4b in 35 cases of BCC tissue arrays and 19 cases of normal human skin tissue was studied using an immunohistochemical approach.
RESULTS: The expression of p15INK4b was not significantly different in the BCC cases as compared with normal human skin (p=0.356; p>0.05). In addition, there were no significant relationship between clinicopathologic variables of patients (age and sex) and p15INK4b protein expression.
CONCLUSIONS: Our finding may indicate that p15INK4b protein expression does not play a role in the genesis of BCC.

Matched MeSH terms: Skin/metabolism
Effect of limonene on permeation enhancement of ketoprofen in palm oil esters nanoemulsion

Sakeena MH, Elrashid SM, Muthanna FA, Ghassan ZA, Kanakal MM, Laila L, et al.

J Oleo Sci, 2010;59(7):395-400.
PMID: 20513974

This study sets out to investigate the in vitro permeation of ketoprofen from the formulated nanoemulsions through excised rat skin. In vitro permeation of ketoprofen nanoemulsion through rat skin was evaluated in Franz diffusion cells and compared with marketed product (Fastum gel). Limonene which has been reported to be a good enhancer for ketoprofen was selected. Moreover the effects of limonene which was added to the nanoemulsion formulations at levels of 1%, 2%, 3% and on rat skin permeation of ketoprofen were also evaluated. The selected optimized formulation was further studied for skin irritation. Utilization of limonene as a penetration enhancer increased the permeation of ketoprofen from the formulated nanoemulsion with increasing concentrations of limonene. The results obtained showed that nanoemulsion with 3% limonene produced similar and comparable skin permeation of ketoprofen with marketed formulation and the skin irritation study on rats showed the optimized formulation prepared was safe.

Matched MeSH terms: Skin/metabolism*
Fulltext Effect of compositions in nanostructured lipid carriers (NLC) on skin hydration and occlusion

Loo Ch, Basri M, Ismail R, Lau H, Tejo B, Kanthimathi M, et al.

Int J Nanomedicine, 2013;8:13-22.
PMID: 23293516 DOI: 10.2147/IJN.S35648

To study the effects of varying lipid concentrations, lipid and oil ratio, and the addition of propylene glycol and lecithin on the long-term physical stability of nanostructured lipid nanocarriers (NLC), skin hydration, and transepidermal water loss.

Matched MeSH terms: Skin/metabolism
Oxidative stress in mouse skin following application of contact allergenic 5-chloro-2-methyl-4-isothiazolin-3-one and oxazolone

Chung LY

Contact Derm., 2005 Mar;52(3):170-1.
PMID: 15811043
Matched MeSH terms: Skin/metabolism
Nanocarriers and their Actions to Improve Skin Permeability and Transdermal Drug Delivery

Khan NR, Harun MS, Nawaz A, Harjoh N, Wong TW

Curr Pharm Des, 2015;21(20):2848-66.
PMID: 25925113

Transdermal drug delivery is impeded by the natural barrier of epidermis namely stratum corneum. This limits the route to transport of drugs with a log octanol-water partition coefficient of 1 to 3, molecular weight of less than 500 Da and melting point of less than 200°C. Nanotechnology has received widespread investigation as nanocarriers are deemed to be able to fluidize the stratum corneum as a function of size, shape, surface charges, and hydrophilicity-hydrophobicity balance, while delivering drugs across the skin barrier. This review provides an overview and update on the latest designs of liposomes, ethosomes, transfersomes, niosomes, magnetosomes, oilin- water nanoemulsions, water-in-oil nanoemulsions, bicontinuous nanoemulsions, covalently crosslinked polysaccharide nanoparticles, ionically crosslinked polysaccharide nanoparticles, polyelectrolyte coacervated nanoparticles and hydrophobically modified polysaccharide nanoparticles with respect to their ability to fuse or fluidize lipid/protein/tight junction regimes of skin, and effect changes in skin permeability and drug flux. Universal relationships of nanocarrier size, zeta potential and chemical composition on transdermal permeation characteristics of drugs will be developed and discussed.

Matched MeSH terms: Skin/metabolism*
A feasibility study: in vivo x-ray fluorescence of iron using 109Cd

Shukri A, Green S, Bradley DA

Appl Radiat Isot, 1995 6 1;46(6-7):625.
PMID: 7633384
Matched MeSH terms: Skin/metabolism
Nanoparticle-based therapies as a modality in treating wounds and preventing biofilm

Dua K, Gupta G, Chellapan DK, Bebawy M, Collet T

Panminerva Med, 2018 Dec;60(4):237-238.
PMID: 30563307 DOI: 10.23736/S0031-0808.18.03435-3
Matched MeSH terms: Skin/metabolism
Sea cucumber (Stichopus hermanii) based hydrogel to treat burn wounds in rats

Zohdi RM, Zakaria ZA, Yusof N, Mustapha NM, Abdullah MN

J Biomed Mater Res B Appl Biomater, 2011 Jul;98(1):30-7.
PMID: 21504052 DOI: 10.1002/jbm.b.31828

Malaysian sea cucumber was incorporated into hydrogel formulation by using electron beam irradiation technique and was introduced as novel cross-linked Gamat Hydrogel dressing. This study investigated whether Gamat Hydrogel enhanced repair of deep partial skin thickness burn wound in rats and its possible mechanism. Wounds were treated with either Gamat Hydrogel, control hydrogel, OpSite® film dressing or left untreated. Skin samples were taken at 7, 14, 21, and 28 days post burn for histological and molecular evaluations. Gamat Hydrogel markedly enhanced wound contraction and improved histological reorganization of the regenerating tissue. Furthermore, the dressing modulated the inflammatory responses, stimulated the activation and proliferation of fibroblasts, and enhanced rapid production of collagen fiber network with a consequently shorter healing time. The level of proinflammatory cytokines; IL-1α, IL-1β, and IL-6, were significantly reduced in Gamat Hydrogel treated wounds compared with other groups as assessed by reverse transcription-polymerase chain reaction (RT-PCR). In summary, our results showed that Gamat Hydrogel promoted burn wound repair via a complex mechanism involving stimulation of tissue regeneration and regulation of pro-inflammatory cytokines. The resultant wound healing effects were attributed to the synergistic effect of the hydrogel matrix and incorporated sea cucumber.

Matched MeSH terms: Skin/metabolism
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/metabolism
Fulltext Molecular Mechanisms of Stress-Responsive Changes in Collagen and Elastin Networks in Skin

Aziz J, Shezali H, Radzi Z, Yahya NA, Abu Kassim NH, Czernuszka J, et al.

Skin Pharmacol Physiol, 2016;29(4):190-203.
PMID: 27434176 DOI: 10.1159/000447017

Collagen and elastin networks make up the majority of the extracellular matrix in many organs, such as the skin. The mechanisms which are involved in the maintenance of homeostatic equilibrium of these networks are numerous, involving the regulation of genetic expression, growth factor secretion, signalling pathways, secondary messaging systems, and ion channel activity. However, many factors are capable of disrupting these pathways, which leads to an imbalance of homeostatic equilibrium. Ultimately, this leads to changes in the physical nature of skin, both functionally and cosmetically. Although various factors have been identified, including carcinogenesis, ultraviolet exposure, and mechanical stretching of skin, it was discovered that many of them affect similar components of regulatory pathways, such as fibroblasts, lysyl oxidase, and fibronectin. Additionally, it was discovered that the various regulatory pathways intersect with each other at various stages instead of working independently of each other. This review paper proposes a model which elucidates how these molecular pathways intersect with one another, and how various internal and external factors can disrupt these pathways, ultimately leading to a disruption in collagen and elastin networks.

Matched MeSH terms: Skin/metabolism*
Recent Update on Nanoemulgel as Topical Drug Delivery System

Choudhury H, Gorain B, Pandey M, Chatterjee LA, Sengupta P, Das A, et al.

J Pharm Sci, 2017 07;106(7):1736-1751.
PMID: 28412398 DOI: 10.1016/j.xphs.2017.03.042

Being an emerging transdermal delivery tool, nanoemulgel, has proved to show surprising upshots for the lipophilic drugs over other formulations. This lipophilic nature of majority of the newer drugs developed in this modern era resulting in poor oral bioavailability, erratic absorption, and pharmacokinetic variations. Therefore, this novel transdermal delivery system has been proved to be advantageous over other oral and topical drug delivery to avoid such disturbances. These nanoemulgels are basically oil-in-water nanoemulsions gelled with the use of some gelling agent in it. This gel phase in the formulation is nongreasy, which favors user compliance and stabilizes the formulation through reduction in surface as well as interfacial tension. Simultaneously, it can be targeted more specifically to the site of action and can avoid first-pass metabolism and relieve the user from gastric/systemic incompatibilities. This brief review is focused on nanoemulgel as a better topical drug delivery system including its components screening, formulation method, and recent pharmacokinetic and pharmacodynamic advancement in research studies carried out by the scientists all over the world. Therefore, at the end of this survey it could be inferred that nanoemulgel can be a better and effective drug delivery tool for the topical system.

Matched MeSH terms: Skin/metabolism
In Vitro and In Vivo Skin Distribution of 5α-Reductase Inhibitors Loaded Into Liquid Crystalline Nanoparticles

Madheswaran T, Baskaran R, Yoo BK, Kesharwani P

J Pharm Sci, 2017 11;106(11):3385-3394.
PMID: 28652158 DOI: 10.1016/j.xphs.2017.06.016

In this study, we developed positively charged liquid crystalline nanoparticles (LCN) coated with chitosan (CHI) to enhance the skin permeation and distribution of 5α-reductase inhibitors for the treatment of androgenetic alopecia. LCN and surface-modified LCN (CHI-LCN) were prepared by ultrasonication method, and their physicochemical properties were characterized. In vitro and in vivo skin permeation and retention were studied using porcine abdominal skin and mice skin using the Franz diffusion cell. Skin distribution and cellular uptake of LCN and CHI-LCN were also investigated. The particle size and surface charge were 244.9 ± 2.1 nm and -19.2 ± 1.1 mV, respectively, for LCNs and 300.0 ± 7.6 nm and 24.7 ± 2.4 mV, respectively, for CHI-LCN. The permeation of 5α-reductase inhibitors was significantly greater with CHI-LCN compared with LCN, whereas there was no significant difference observed in the skin distribution. In fluorescence studies, fluorescence intensity was higher for CHI-LCNs throughout the skin, whereas more intense fluorescence was seen only in the epidermis layer for LCN. CHI-LCN showed greater cellular uptake than LCN, resulting in internalization of 98.5 ± 1.9% of nanoparticles into human keratinocyte cells. In conclusion, surface modification of LCN with CHI is a promising strategy for increasing skin permeation of 5α-reductase inhibitors for topical delivery.

Matched MeSH terms: Skin/metabolism

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