Many properties of chemicals depend on their stereochemistry. Among these, the effects of stereoisomerism on percutaneous absorption of drugs are not well studied. We have previously shown that permeation of tretinoin and isotretinoin (two geometric isomers) through hydrophilic enhancers-treated rat skin is stereoselective. As, depending on their lipophilicity, penetration enhancers can change ...

Many properties of chemicals depend on their stereochemistry. Among these, the effects of stereoisomerism on percutaneous absorption of drugs are not well studied. We have previously shown that permeation of tretinoin and isotretinoin (two geometric isomers) through hydrophilic enhancers-treated rat skin is stereoselective. As, depending on their lipophilicity, penetration enhancers can change ...

The permeability of the cornea to drugs is clinically important because it is the major factor determining the efficacy of topically applied ophthalmic preparations. With this perspective, the present article gives a brief update and overview of corneal structure and proposed mechanisms of permeation. Physiological, physicochemical and formulation factors affecting drug permeation through corne...

Antimicrobial therapy remains to be the most important method of wound infection treatment. Systemically administered antimicrobials may not achieve therapeutic level in wound. On the other hand, in the absence of surgical debridement (due to any reason), most topically applied antimicrobials cannot penetrate the wound in therapeutic amount due to the presence of eschar. Burn eschar is a protei...

KEY POINTS Kainate receptor heteromerization and auxiliary subunits, Neto1 and Neto2, attenuate polyamine ion-channel block by facilitating blocker permeation. Relief of polyamine block in GluK2/GluK5 heteromers results from a key proline residue that produces architectural changes in the channel pore α-helical region. Auxiliary subunits exert an additive effect to heteromerization, and thus re...

the aim of the present study was to investigate the relationship between the polar surface area and other molecular properties of the model drugs and their transdermal permeability across the rat skin. few model drugs which are weakly acidic (ibuprofen, aceclofenac and glipizide) and weakly basic (olanzapine, telmisartan and sildenafil citrate) were selected for the study based on polar surface...

formulation by using chemical penetration enhancers and to study the effect of pulsed current on permeation through guinea pig, Wistar rat and human cadaver skin. Modified Franz diffusion cell was used to study the in vitro permeation across various types of skin by iontophoresis. The thermo-reversible gel was prepared and optimized by cold method using poloxamer 407 as a gelling agent. Thermo-...

a broad range of per-meation events from femtoseconds to minutes in time scale and sub-angstrom to millimeter in space were discussed. A main message in the Perspectives was to explore each discipline to expand its limitation, such that different levels of knowledge in a hierarchy of ion permeation events are integrated. Here, we propose another approach from a mesoscopic point of view. Electro...

Infection is the primary source of mortality in burn patients. One of the main treatment methods of burn wound infections is topical antimicrobial therapy, in which drugs have to permeate a dead tissue called eschar. Unfortunately, most antimicrobial agents can not permeate eschar in therapeutic levels. Surprisingly, permeation properties of this barrier and effects of chemical or environmental...

Infection is the primary source of mortality in burn patients. One of the main treatment methods of burn wound infections is topical antimicrobial therapy, in which drugs have to permeate a dead tissue called eschar. Unfortunately, most antimicrobial agents can not permeate eschar in therapeutic levels. Surprisingly, permeation properties of this barrier and effects of chemical or environmental...