Recent developments in topical and transdermal delivery

Hadgraft, Jonathan

doi:10.1007/bf03190266

Cited by 59 publications

(36 citation statements)

References 29 publications

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“…EtOH is known to irritate skin and delipidate surface membranes (Scheuplein and Blank, 1973;Finnin and Morgan, 1999) which may contribute to penetration of dissolved substances through the skin. Similarly, PG has been shown to diffuse into skin and improve the solubility of skin lipids to the diffusant (Hadgraft, 1996). Since many commercially available topical preparations contain alcohol and/or PG as components of the cream base (Thomas, 2002), the relative proportion of vehicle constituents may also affect the transdermal penetration of testosterone.…”

Section: Discussionmentioning

confidence: 98%

“…Maximum flux (J max , mol cm −2 h −1 ) was predicted from k P multiplied by the solubility in the donor phase. In aqueous solutions, J max estimates the total amount of drug penetration possible per unit time from a saturated solution as the product of skin area, k P and aqueous solubility (Hadgraft, 1996). The amount of radiolabelled alcohol remaining within each skin sample at the completion of the study was divided by the donor recovery fraction to adjust for donor depletion.…”

Section: Discussionmentioning

confidence: 99%

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Vehicle Effects on the In Vitro Penetration of Testosterone through Equine Skin

Mills

2006

Vet Res Commun

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The effects of three vehicles, phosphate-buffered saline (PBS), ethanol (50% in PBS w/w) and propylene glycol (50% in PBS w/w) on in vitro transdermal penetration of testosterone was investigated in the horse. Skin was harvested from the thorax of five Thoroughbred horses after euthanasia and stored at -20 degrees C until required. The skin was then defrosted and placed into Franz-type diffusion cells, which were maintained at approximately 32 degrees C by a water bath. Saturated solutions of testosterone, containing trace amounts of radiolabelled [14C]testosterone, in each vehicle were applied to the outer (stratum corneum) surface of each skin sample and aliquots of receptor fluid were collected at 0, 2, 4, 8, 16, 20, 22 and 24 h and analysed for testosterone by scintillation counting. The maximum flux (Jmax) of testosterone was significantly higher for all sites when testosterone was dissolved in a vehicle containing 50% ethanol or 50% propylene glycol, compared to PBS. In contrast, higher residues of testosterone were found remaining within the skin when PBS was used as a vehicle. This study shows that variability in clinical response to testosterone could be expected with formulation design.

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Section: Discussionmentioning

confidence: 98%

Section: Discussionmentioning

confidence: 99%

Vehicle Effects on the In Vitro Penetration of Testosterone through Equine Skin

Mills

2006

Vet Res Commun

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“…In search of a vehicle to deliver the medicament into the skin layers (cutaneous delivery), or through the skin and into the systemic circulation (percutaneous absorption), varied kinds of formulation systems and strategies have been evolved. [1][2][3][4][5][6] Among the many, the lipid-based formulations have been in use for decades. [7][8][9][10][11] However, of late, there has been a surge in their number with wide variation and flexibility in the interior designs and structures.…”

Section: Introductionmentioning

confidence: 99%

Lecithin organogels as a potential phospholipid-structured system for topical drug delivery: A review

2005

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The purpose of this review is to give an insight into the considerable potential of lecithin organogels (LOs) in the applications meant for topical drug delivery. LOs are clear, thermodynamically stable, viscoelastic, and biocompatible jelly-like phases, chiefly composed of hydrated phospholipids and appropriate organic liquid. These systems are currently of interest to the pharmaceutical scientist because of their structural and functional benefits. Several therapeutic agents have been formulated as LOs for their facilitated transport through topical route (for dermal or transdermal effect), with some very encouraging results. The improved topical drug delivery has mainly been attributed to the biphasic drug solubility, the desired drug partitioning, and the modification of skin barrier function by the organogel components. Being thermodynamically stable, LOs are prepared by spontaneous emulsification and therefore possess prolonged shelf life. The utility of this novel matrix as a topical vehicle has further increased owing to its very low skin irritancy potential. Varied aspects of LOs viz formation, composition, phase behavior, and characterization have been elaborated, including a general discussion on the developmental background. Besides a comprehensive update on the topical applications of lecithin organogels, the review also includes a detailed account on the mechanistics of organogelling.

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“…In an ideal system, there is a linear relationship between the rate of diffusion and the concentration of diffusant. The maximum flux occurs when the concentration reaches the solubility limit [21]. The cumulative ASA permeated was further increased to 404.49 ± 2.3 µg/cm 2 (patch IIc) on increasing drug load to 50 mg/patch.…”

Section: In Vitro Permeation Of Asa From the Transdermal Patches Contmentioning

confidence: 86%

Effect of Transdermally Delivered Aspirin on Blood Coagulation Parameters

Shamsher¹,

Charoo²,

Kohli³

et al. 2010

Am. J. Biomed. Sci.

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The efficacy of oral aspirin treatment in the secondary prevention of cardio and cerebro vascular disease is well known. However oral administration is often associated with abdominal discomfort. The feasibility of delivering aspirin transdermally from eudragit and polyvinyl acetate (PVA) matrix-type patches to enhance its antithrombotic efficiency of aspirin was investigated. Transdermal films containing mixture of eudragit RL: eudragit RS and polyvinyl acetate were fabricated. Eudragit RL: eudragit RS (5:1) films containing 30 mg/ transdermal patch aspirin showed maximum release (11.891.1g/cm 2 ) after 24 hrs as compared to PVA films. With regards to appearance eudragit films were also wrinkle free, uniform, flexible and transparent with good adhesion property to skin. The effect of turpentine oil and lemon oil at different concentrations on the in vitro percutaneous absorption of aspirin from eudragit copolymer patches through rat skin was investigated. Two formulation containing 50 mg/transdermal patch ASA with 0.042 ml turpentine oil and 0.042 ml lemon oil showed a significantly higher flux of ASA 4.22 g/cm 2 /hr and 38.52 g/cm 2 /hr respectively. The optimized formulations influenced the blood coagulation parameters (bleeding time, prothrombin time, Activated partial prothrombin time) significantly by means of affecting both the extrinsic coagulation system and the intrinsic coagulation system as compared to orally administered and control gel formulations.

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Recent developments in topical and transdermal delivery

Cited by 59 publications

References 29 publications

Vehicle Effects on the In Vitro Penetration of Testosterone through Equine Skin

Vehicle Effects on the In Vitro Penetration of Testosterone through Equine Skin

Lecithin organogels as a potential phospholipid-structured system for topical drug delivery: A review

Effect of Transdermally Delivered Aspirin on Blood Coagulation Parameters

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