Codiffusion of propylene glycol and dimethyl isosorbide in hairless mouse skin

Squillante, Emilio; Needham, Thomas E.; Maniar, Anita; Kislalioglu, Serpil M.; Zia, Hossein

doi:10.1016/s0939-6411(98)00030-7

Cited by 38 publications

(26 citation statements)

References 15 publications

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“…Long-chain fatty acids and other hydrophobic enhancers have been applied in combination with a relatively hydrophilic vehicle, such as PG, to achieve an enhanced penetration effect (60). This synergistic enhancement is probably due to the facilitated incorporation of a fatty acid (i.e., oleic acid) into the stratum corneum lipid alkyl domain by the interaction of PG at the polar head group region (61), facilitating the permeation of drugs through the skin (62). As shown in the present paper, the concentration of PG (20.0%, w/w) used in the delivery systems must promote a synergic effect with OA, thus contributing to the increase of the drug permeation flux (J) through the skin.…”

Section: Discussionmentioning

confidence: 99%

A Novel Transdermal Delivery System for the Anti-Inflammatory Lumiracoxib: Influence of Oleic Acid on In Vitro Percutaneous Absorption and In Vivo Potential Cutaneous Irritation

2010

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Abstract. Transdermal delivery of non-steroidal anti-inflammatory drugs may be an interesting strategy for delivering these drugs to the diseased site, but it would be ineffective due to low skin permeability. We investigated whether oleic acid (OA), a lipid penetration enhancer in poloxamer gels named poloxamer-based delivery systems (PBDS), can improve lumiracoxib (LM) delivery to/through the skin. The LM partition coefficient (K) studies were carried out in order to evaluate the drug lipophilicity grade (K octanol/buffer ), showing values >1 which demonstrated its high lipophilicity. Both in vitro percutaneous absorption and skin retention studies of LM were measured in the presence or absence of OA (in different concentrations) in PBDS using porcine ear skin. The flux of in vitro percutaneous absorption and in vitro retention of LM in viable epidermis increased in the presence of 10.0% (w/w) OA in 25.0% (w/w) poloxamer gel. In vivo cutaneous irritation potential was carried out in rabbits showing that this formulation did not provide primary or cumulative cutaneous irritability in animal model. The results showed that 25.0% poloxamer gel containing 10.0% OA is potential transdermal delivery system for LM.KEY WORDS: in vitro skin permeation; lumiracoxib; oleic acid; poloxamer-based delivery systems; skin delivery.

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Section: Discussionmentioning

confidence: 99%

A Novel Transdermal Delivery System for the Anti-Inflammatory Lumiracoxib: Influence of Oleic Acid on In Vitro Percutaneous Absorption and In Vivo Potential Cutaneous Irritation

2010

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“…26,27) In this study, it was observed that the drug release rate from the film formulations containing NFD in concentrations of 3 to 10% was between 792 µg/cm 2 /h and 1189 µg/cm 2 /h. These values were very high when compared with the value predicted for the permeation of NFD through the skin.…”

Section: Mechanical Properties Of Transdermal Filmsmentioning

confidence: 71%

“…Propylene glycol, cis-oleic acid, dimethyl isosorbide and d-limonene as permeation enhancer were used in order to enhance its transdermal permeation in literature. [24][25][26][27] The aim of the present study was to design matrix-type transdermal films of NFD with pectin and sodium alginate, which are polysaccharide-based polymers, and to assess their mechanical properties such as tensile strength and elasticity, as well as the in vitro permeation of NFD across excised rat skin from transdermal films containing nerolidol as penetration enhancer.…”

Section: )mentioning

confidence: 99%

Design and Evaluation of Polysaccharide-Based Transdermal Films for the Controlled Delivery of Nifedipine

Bektaş

Cevher

Güngör

et al. 2014

CHEMICAL & PHARMACEUTICAL BULLETIN

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It was aimed to develop the matrix type polysaccharide-based transdermal films of nifedipine (NFD) to provide its long term plasma concentration. The mechanical tests were carried out on gel formulations which were utilised in the fabrication of transdermal films to determine the type of polymer (pectin, sodium alginate) and plasticizer (propylene glycol, glycerine) as well as their concentrations. The mechanical strength, elasticity, bioadhesiveness and the drug release characteristics of optimised films containing NFD were evaluated. Permeation of NFD from the films with/without adding an enhancer (nerolidol) was followed through excised rat skin using Franz diffusion cells. Results showed that the gels composed of either pectin or sodium alginate were appropriate for the fabrication of transdermal films of NFD, and the addition of propylene glycol improved mechanical strength, flexibility, and bioadhesiveness of the films. Permeation data showed that nerolidol was an effective permeation enhancer for the polysaccharide-based transdermal films of NFD.Key words nifedipine; transdermal film; sodium alginate; pectin; texture analysis; nerolidol Transdermal delivery possesses many advantages over conventional drug administration routes, including avoidance of intestinal and/or hepatic first pass metabolism, reduction in side effects and better patient compliance. Polymers are crucial components for the formulation of transdermal delivery systems. There are some critical parameters for the optimisation of transdermal therapeutic systems including physical or chemical stability of the formulation, compatibility with skin, adhesion to skin, the release characteristics of drug from the vehicle and its permeation through the skin. Therefore, the choice of polymers and plasticizers used in transdermal systems have strong impact on drug release, permeability, elasticity, and wearing properties of transdermal formulations. 1,2)Natural polysaccharides such as sodium alginate, chitosan, pectin, guar gum, gellan gum have been widely evaluated as a polymer in the optimisation of transdermal systems due to their non-toxic, biocompatible and potentially biodegradable properties.3,4) Sodium alginate is a mixture of polyuronic acids composed of residues of D-mannuronic acid and L-guluronic acid, which is used in design of controlled drug delivery formulations.5) It has also been used to formulate transdermal films. 6,7)Despite all the advantages of transdermal drug delivery, stratum corneum, the outermost layer of the skin, provides the greatest resistance to entrance of drugs to the systemic blood stream. In order to achieve therapeutic drug concentration following transdermal administration, penetration enhancers which reduce the barrier characteristics of stratum corneum reversibly are added into transdermal formulations. 8,9)Terpenes appear to have good skin penetration characteristics for transdermal systems due to their low cutaneous irritancies, good toxicological profiles.8) Moreover, this interaction with the stratum cor...

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“…33) In addition, PG readily permeates the skin and in doing so, it might have carried the drug molecules across. 34) Moreover, use of this co-solvent in combination with enhancers like fatty alcohols (in this case, the enzymatically released free fatty alcohols) or fatty esters (prodrugs themselves) offers synergistic enhancing effect for ketorolac. 22,[35][36][37] During study, KS and ketorolac were saturated in PG in order to keep a constant driving force with maximum thermodynamic activity.…”

Section: Discussionmentioning

confidence: 99%

Evaluation of Physicochemical Properties, Skin Permeation and Accumulation Profiles of Ketorolac Fatty Ester Prodrugs

Bhandari

Newa

Yoon

et al. 2007

Biological & Pharmaceutical Bulletin

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Deep tissue accumulation and systemic absorption is not the aim of local topical medication. Unfortunately, most of the disorders requiring such medication are found in the area of high permeation flux and in most cases, stratum corneum (SC) barrier resistance is decreased allowing their easier permeation in order to attain plasma levels that could be sufficient to elicit adverse reactions.1) There have been many attempts to develop a suitable approach to minimize their systemic absorption and the resulting adverse effects. More recently, there has been interest in agents that may be used in topical formulations to prevent the permeation of active ingredients or excipients.2) But, not all of these permeation retardants have yet been proven to be commercially viable and pharmaceutically suitable and in many cases, retardation has been achieved by compromising systemic and local toxicities of the retarders.3) Therefore, it would be an advantage if the systemic absorption of topical agents could be minimized irrespective of the sites or altered skin barrier function without the co-application of other chemical retarders.It is a well known fact that the permeability barrier properties of skin are mediated by a series of lipid multilayers segregated within SC interstices, and their hydrophobic nature and tortuous, extracellular localization restrict the transport of most compounds across the SC. 4) When this barrier is acutely perturbed by removing lipids with organic solvents, detergents, or tape stripping; a sequence of biological responses is initiated including accelerated epidermal lipid synthesis 5-7) that replenishes the skin lipid content which contribute to rapidly restore the skin barrier function.8) The specific requirement for epidermal lipids to create the barrier has also been delineated using the specific inhibitors of the rate-limiting enzymes of lipid synthesis, [9][10][11][12] and such selective inhibition of the synthesis of one or more of SC lipids increased SC permeability to epicutaneously applied drugs.13) Topical application of 5-(tetradecyloxy)-2-furancarboxylic acid (TOFA)-the rate limiting enzymes of fatty acid synthesis-immediately after barrier disruption inhibited the early stages of barrier recovery due to deletion of the target lipid from the extracellular membranes. But, the barrier recovery was normalized, and abnormalities in lamellar body and SC membrane structure were corrected by the co-application of palmitate (C16:0 fatty ester) with TOFA, indicating that the delay was due to the deficiency in bulk lipids.9-12) In addition, previous studies about the role of SC lipids as the determinant of the permeability barrier to the drug penetration reported an inverse correlation between the solute penetration and the total SC lipid weight (neither the number of cell layers nor the thickness of the SC correlated with the observed differences in permeability), 14,15) and showed that the enhanced epidermal lipid synthesis in SC or providing exogenous lipids resulted into a more efficient ba...

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Codiffusion of propylene glycol and dimethyl isosorbide in hairless mouse skin

Cited by 38 publications

References 15 publications

A Novel Transdermal Delivery System for the Anti-Inflammatory Lumiracoxib: Influence of Oleic Acid on In Vitro Percutaneous Absorption and In Vivo Potential Cutaneous Irritation

A Novel Transdermal Delivery System for the Anti-Inflammatory Lumiracoxib: Influence of Oleic Acid on In Vitro Percutaneous Absorption and In Vivo Potential Cutaneous Irritation

Design and Evaluation of Polysaccharide-Based Transdermal Films for the Controlled Delivery of Nifedipine

Evaluation of Physicochemical Properties, Skin Permeation and Accumulation Profiles of Ketorolac Fatty Ester Prodrugs

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