Estimation of intradermal disposition kinetics of drugs: II. Factors determining penetration of drugs from viable skin to muscular layer

Higaki, Kazutaka; Asai, Masahide; Suyama, Takayuki; Nakayama, Kazuki; Ogawara, Ken Ichi; Kimura, Toshikiro

doi:10.1016/s0378-5173(02)00084-4

Cited by 38 publications

(36 citation statements)

References 19 publications

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“…Buspirone has a low aqueous solubility and is a highly lipophilic diffusant (21,61,62). Bupivacaine is a moderately lipophilic diffusant with a log D value of 2.48 at a pH of 6.8 (63,64). These lipophilic diffusants preferentially transverse across the lipophilic cell membrane, and the route is called the transcellular route (trans-across).…”

Section: Discussionmentioning

confidence: 99%

Effect of Experimental Temperature on the Permeation of Model Diffusants Across Porcine Buccal Mucosa

Kulkarni

Ravichandran

et al. 2011

AAPS PharmSciTech

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Abstract. The influence of experimental temperature on the permeability of model diffusants across porcine buccal mucosa was investigated in vitro. The permeability increased significantly as the experimental temperature was increased in increments of approximately 7°C. It was observed that the apparent permeability and temperature were related by an exponential relationship that conformed to the Arrhenius equation. Diffusants with higher lipophilicities-buspirone and bupivacaine-had lower activation energies for diffusion when compared to hydrophilic diffusants-antipyrine and caffeine. The activation energy for diffusion of the model diffusants decreased linearly with increasing distribution coefficients across porcine buccal mucosa. The results suggested that the buccal mucosa acts as a stronger barrier to the diffusion of hydrophilic diffusants than the lipophilic ones. The log-linear relationship between permeability and temperature indicates that temperature should be carefully controlled in diffusion experiments. These results also point to the possibility of developing heat-generating buccal delivery devices, especially for hydrophobic diffusants.

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Section: Discussionmentioning

confidence: 99%

Effect of Experimental Temperature on the Permeation of Model Diffusants Across Porcine Buccal Mucosa

Kulkarni

Ravichandran

et al. 2011

AAPS PharmSciTech

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“…These included three acidic (naproxen, warfarin, nimesulide), seven basic (lidocaine, propranolol, verapamil, diltiazem, amitriptyline, metoprolol, pindolol), and two neutral (caffeine, antipyrine) molecules. LogP and logD 6.8 (log 10 of distribution coefficient at pH 6.8, which corresponds to salivary pH) values were obtained either from literature or were estimated using ChemIDplus (8)(9)(10)(11)(12)(13)(14)(15). Drugs with a logD 6.8 value of greater than −1.0 and lower than +1.0 were selected as model compounds to minimize the effects of unstirred water layer and drug accumulation in the membrane.…”

Section: Drugs and Descriptorsmentioning

confidence: 99%

Effect of Drug Lipophilicity and Ionization on Permeability Across the Buccal Mucosa: A Technical Note

Kokate

Jasti

2008

AAPS PharmSciTech

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“…36 In addition, the penetration or bioavailability rate of topically applied drugs is dependent on the thermodynamic activity of the drug in the vehicle if specific penetration enhancers are absent. 37 However, in formulations in which penetration enhancers are used, penetration enhancement and thermodynamic effects are both expected to influence drug flux. 38 Only aqueous suspensions lead to equivalent, or in this case, maximum thermodynamic activity.…”

Section: Discussionmentioning

confidence: 99%

Amphiphilic star-like macromolecules as novel carriers for topical delivery of nonsteroidal anti-inflammatory drugs

2003

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KEYWORDS: topical drug delivery, NSAIDs, polymeric micelle, permeation, drug releaseThe objective of this study was to evaluate amphiphilic star-like macromolecules (ASMs) as a topical drug delivery system. Indomethacin, piroxicam, and ketoprofen were individually encapsulated into the ASMs using coprecipitation. The effects of the ASMs on percutaneous permeation of nonsteroidal anti-inflammatory drugs (NSAIDs) across full thickness, hairless mouse skin were evaluated in vitro using modified Franz diffusion cells. In addition, solubility and in vitro release experiments were performed to characterize ASMs behavior in aqueous media. Poly(ethylene glycol) (PEG) and Pluronic P-85 were used as polymer controls to compare the role of PEG and amphiphilic behavior in the ASMs. In vitro release experiments indicated that ASMs can delay drug release (P < .05), whereas solubility measurements showed that ASMs can increase NSAIDs aqueous solubility (P < .05). Percutaneous permeation studies revealed that ASMs decreased both flux and Q 24 of drugs compared with the control (P < .10). Skin pretreatment studies with ASMcontaining solution before drug application demonstrated that pretreatment similarly influenced NSAID percutaneous permeation. In conclusion, ASMs likely slow drug permeation through 2 mechanisms, delayed drug diffusion from its core and skin dehydration by its shell. Thus, ASMs may be useful for delayed dermal delivery or prevention of compound permeation through the skin (eg, sunscreens, N,N-diethyl-mtoluamide [DEET]) from aqueous formulations.

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Estimation of intradermal disposition kinetics of drugs: II. Factors determining penetration of drugs from viable skin to muscular layer

Cited by 38 publications

References 19 publications

Effect of Experimental Temperature on the Permeation of Model Diffusants Across Porcine Buccal Mucosa

Effect of Experimental Temperature on the Permeation of Model Diffusants Across Porcine Buccal Mucosa

Effect of Drug Lipophilicity and Ionization on Permeability Across the Buccal Mucosa: A Technical Note

Amphiphilic star-like macromolecules as novel carriers for topical delivery of nonsteroidal anti-inflammatory drugs

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