Cultured skin loaded with tetracycline HCl and chloramphenicol as dermal delivery system: Mathematical evaluation of the cultured skin containing antibiotics

Hada, Nobuko; Hasegawa, Tetsuya; Takahashi, Hidekazu; Ishibashi, Takuya; Sugibayashi, Kenji

doi:10.1016/j.jconrel.2005.08.020

Cited by 26 publications

(19 citation statements)

References 21 publications

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“…However, it is important to note that the water-impermeable barrier function of the model we used is weaker than that of intact human skin (9). Thus, the results of the present study do not necessarily indicate that cortisol synthesis and secretion would be increased by environmental dryness in healthy normal human skin.…”

Section: Discussionmentioning

confidence: 55%

Low environmental humidity induces synthesis and release of cortisol in an epidermal organotypic culture system

Takei

Denda

Kumamoto

et al. 2013

Experimental Dermatology

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Dry environmental conditions induce a variety of skin pathologies and a recent report indicating that cortisol synthesis in epidermis was increased during wound healing led us to hypothesize that environmental dryness might induce increased cortisol secretion in epidermis. Therefore, we incubated a skin equivalent model under dry (relative humidity: less than 10%) and humid (relative humidity: approximately 100%) conditions for 48 hours and evaluated cortisol secretion and mRNA levels of cortisol-synthesizing enzyme (steroid 11b-hydroxylase, CYP11B1) and IL-1b. Cortisol secretion was increased threefold, and CYP11B1 and IL-1b mRNAs were increased 38-fold and sixfold, respectively, in the dry condition versus the humid condition.Occlusion with a water-impermeable plastic membrane partially blocked the increases in cortisol secretion and CYP11B1 and IL-1b mRNA expression in the dry condition. Thus, environmental dryness might induce increased cortisol secretion in epidermis of diseased skin characterized by epidermal barrier dysfunction, potentially influencing mental state and systemic physiology.Abbreviations: CYP, cytochrome P450; CYP11B1, steroid 11b-hydroxylase (cortisol-synthesizing enzyme); IL-1b, interleukin 1 beta.

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Section: Discussionmentioning

confidence: 55%

Low environmental humidity induces synthesis and release of cortisol in an epidermal organotypic culture system

Takei

Denda

Kumamoto

et al. 2013

Experimental Dermatology

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“…The thickness of the stratum corneum, L sc , and viable epidermis and dermis, L ved , of LSE-high were 15 and 285 mm, respectively, according to our previous study. 13,15) Figures 5a and b show the time course of the cumulative amount of TA permeated through full-thickness and stripped LSE-high, respectively, after application of 10 mg/ml TA solution and 1000 mg/ml TA suspension. Table 3 summarizes the obtained permeation parameters.…”

Section: Resultsmentioning

confidence: 99%

“…The analytical method was shown in our previous study. 14,15) A one-layered model was used for the silicone membrane and stripped skin (hairless rat, porcine and LSE-high), and a two-layered model was for the full-thickness skin. Figures 1a and b illustrate typical concentration-distance profiles through one-layered and two-layered membrane models, respectively.…”

Section: Theoreticalmentioning

confidence: 99%

Effect of Thermodynamic Activity on Skin Permeation and Skin Concentration of Triamcinolone Acetonide

2010

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Studies on topical formulations containing steroidal drugs were started in 1952 by Goldman et al.,1) who firstly used topical formulations containing a steroid, cortisone acetate, to treat skin diseases. Dumas and Scholtz reported typical concentration dependence of steroidal drugs on the pharmacological effect against psoriasis.2) The effect of topical steroids is closely related to the steroidal concentration at the skin disease site. The skin concentration is usually determined by partition and diffusivity of the steroid into and through the skin. The calculated concentration is sometimes more useful than the directly observed skin concentration.3) The partition and diffusion properties are affected by the thermodynamic activity and state (solution/suspension) of steroids, as well as the barrier function of the skin. Generally, the thermodynamic activity of drugs shows their escaping tendencies from formulations. 4) Skin permeation is a transport phenomenon from a high activity-site to a low activitysite, indicating that skin permeation occurs due to an activity difference. 5) Thermodynamic activity of drugs must be considered when designing topical [6][7][8] and cosmetic formulations. 9) Most studies on steroidal drugs focused on their pharmacological effects, 1,2,10,11) but not on steroid disposition in the skin. 11,12) There are very few studies, however, on the effect of thermodynamic activity and state (solution/suspension) of steroids in topical formulations on skin permeation and skin disposition.A medium strength steroid, triamcinolone acetonide (TA), was selected as a model drug in the present study. The effects of thermodynamic activity and TA state were evaluated for the TA concentration in the stratum corneum and viable epidermis and dermis. One-layered and two layered models were used to analyze the membrane permeation and concentration of TA by Fick's law of diffusion. Distilled water was used as a formulation vehicle to simplify evaluate the effect of thermodynamic activity and TA state. ExperimentalMaterials and Experimental Animals A powder of triamcinolone acetonide (TA) (MW; 434.5, mp; 290°C, Log P; 2.53, solubility in water at 32°C; 22.05Ϯ0.05 mg/ml, and solubility parameter; 9.45 (cal/cm 3 ) 1/2 ) was purchased from Wako Pure Chemical Industries, Ltd. (Chuo, Osaka, Japan). A disposable syringe filter unit (DISMIC ® -13HP 0.20 mm) was purchased from Toyo Roshi Kaisha, Ltd. (Bunkyo, Tokyo, Japan). Other chemicals and solvents were of reagent grade or HPLC grade and used without further purification. A silicone membrane (LTC-S1-75, thickness of 75 mm) was a kind gift from Lintec Co., Ltd. (Itabashi, Tokyo, Japan). A three-dimensional cultured human skin model (LSE-high: TMLSE-003) was purchased from Toyobo Co., Ltd. (Kita, Osaka, Japan). Male hairless rats (WBM/ILA-Ht, 8-9 weeks-old, body weight: 230-260 g) were obtained from the Life Science Research Center, Josai University (Sakado, Saitama, Japan) or Ishikawa Experimental Animals (Fukaya, Saitama, Japan). The animal feeding and experiment...

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“…4 can be changed to Eq. 5, as described in detail by Hada et al 18) and Sugibayashi et al 19) (5) where C ved i, j is FD-4 concentration at i-th position and j-th time in the stripped skin, r is Dt/Dx 2 ; Dx is x iϩ1 Ϫx i , and Dt is t jϩ1 Ϫt j . In addition, the skin permeation rate to the receiver compartment, J, can be expressed by Eq.…”

Section: Analysis Of Diffusivity From Skin Permeation Profilesmentioning

confidence: 99%

Macromolecular Delivery into Skin Using a Hollow Microneedle

Wonglertnirant

Todo

Opanasopit

et al. 2010

Biological & Pharmaceutical Bulletin

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Recently much attention has been paid to a new approach for enhancing transdermal drug delivery employing needles in micron scale, termed microneedles. Such a technique combines the concepts of the user-friendly delivery of transdermal patches and the broad effectiveness of hypodermic injections. Several studies have established the increasing efficacy of microneedle-assisted transdermal delivery for a variety of compounds, [1][2][3][4] especially for high molecular weight hydrophilic compounds. [5][6][7] Microneedles are also expected to be safe, because they are minimally invasive and do not typically cause bleeding or any severe pain at the injection site. 8)Although microneedles assist in penetrating the stratum corneum (SC) barrier and offer several microchannels facilitating drug transport across the skin, the release of macromolecular drugs at the desired therapeutic rate might not be achieved by only (enhanced) passive diffusion from the patch-based drug reservoir due to the small diffusional area produced by needles.9) It is necessary to further improve the transdermal delivery of drugs of large molecular weight by contributing push pressure to propel the drug toward the skin, similar to conventional topical injection. Wu et al. reported that the combination of solid microneedle pretreatment and subsequent iontophoresis significantly enhanced FD flux compared with microneedle pretreatment alone or iontophoresis alone.9)It is difficult, however, to determine the penetration-enhancing effect as well as the parameters affecting the delivery efficiency produced by each enhancing technique and also by each individual microneedle. Yoshida et al. carried out a study to investigate the dermatopharmacokinetics (DPK) and systemic drug disposition after topical (intracutaneous (i.c.)) injection of sodium salicylate and concluded that the injection volume was one of the factors which can be utilized to control the drug migration rate from the injection site.10) Al-Qallaf et al. found that different surface areas of the hollow microneedle array-patch system affected the blood concentration of human growth hormone (hGH). 11)Moreover, information on the effect of several factors related to the delivery efficiency of hollow microneedles, for instance, various needle parameters, including injection conditions (e.g. length of microneedle/injection depth, needle numbers, distance between each needle, hollow size, pressure of injection, etc.), physicochemical properties of drugs (e.g. molecular weight, lipophilicity, etc.), and formulations must be considered for designing the optimum device.In this study, we therefore concentrated only on the influence of variables related to the hollow microneedle system on in vitro drug release behavior from skin. A single 33-gauge hypodermic needle, where the diameter was almost the same to the arrayed microneedles recently reported, 2,7,9,12,13) was used as a single type hollow microneedle in order to reduce the effect of needle parameters. The effects of injection volume and number o...

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Cultured skin loaded with tetracycline HCl and chloramphenicol as dermal delivery system: Mathematical evaluation of the cultured skin containing antibiotics

Cited by 26 publications

References 21 publications

Low environmental humidity induces synthesis and release of cortisol in an epidermal organotypic culture system

Low environmental humidity induces synthesis and release of cortisol in an epidermal organotypic culture system

Effect of Thermodynamic Activity on Skin Permeation and Skin Concentration of Triamcinolone Acetonide

Macromolecular Delivery into Skin Using a Hollow Microneedle

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