Lecithin Organogel as Matrix for Transdermal Transport of Drugs

Willimann, Haus; Walde, Peter; Luisi, Pier Luigi; Gazzaniga, A.; Stroppolo, F.

doi:10.1002/jps.2600810906

Cited by 147 publications

(83 citation statements)

References 11 publications

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“…The micelles grow to a cylindrical or worm-like structure, which tends to give rise to viscous system. 20) In one report about topical delivery of b-blockers using anhydrous SMEDDS composed of surfactant-isopropyl myristate mixture, bupranolol was applied to New Zealand albino rabbits. In their study, the pharmacological activity was improved when water was partitioned into the system from skin, where they discussed this was due to the enhanced diffusion pressure induced by the enhanced thermodynamic activity of bupranolol within the system.…”

Section: Resultsmentioning

confidence: 99%

Design and Evaluation of Prostaglandin E1 (PGE1) Intraurethral Liquid Formulation Employing Self-Microemulsifying Drug Delivery System (SMEDDS) for Erectile Dysfunction Treatment

Lee

Choi

2008

Biological & Pharmaceutical Bulletin

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Erectile dysfunction is a common disease that affects approximately 10% of adult men in the world.1) It impairs sexual performance, diminishes self-esteem and disrupts personal relationship.2) It becomes more frequent with age but it is not an inevitable consequence of normal aging. 3)Since 1983, several products for the treatment of erectile dysfunction such as injection formulations of phenoxybenzamin, papaverin hydrochloride, phentolamin mesylate and prostaglandin E 1 , intended to be injected into the corpus cavernosum were introduced. However, the intracorporeal injection of these products has occasionally been accompanied by the side effects such as pain, priapism, penile hematomas and fibrosis. For these reasons, up to 50% of erectile dysfunction patients using intracavernous injection therapy eventually discontinue the treatment. 2,[4][5][6] Up to now, prostaglandin E 1 (PGE 1 ) has been known as one of the most potent compounds used as a single-dose pharmacotherapy for erectile dysfunction 7) generally administered by intracavernosal injection (e.g., Caverject ® , Pfizer). PGE 1 increases the intracellular concentration of 3Ј,5Ј-cyclic adenosine monophosphate (cAMP) by activation of specific membrane receptors that interact with stimulatory guanine nucleotide proteins to trigger adenylate cyclase and elevate intracellular cAMP concentration.8) Increasing the intracellular cAMP concentration induces the relaxation of arterial and trabecular smooth muscle in the corpus cavernosum and thereby causes penile erection. 7)A non-invasive intraurethral PGE 1 suppository (MUSE ® , Vivus Inc.) has been introduced as a more convenient and safer formulation compared to the injection type of PGE 1 . 1)However, intraurethral suppository formulation may cause some discomforts including feeling of foreign body and pain mainly exhibited by bulky insertion device. 9,10) For this reason, we attempted to develop a novel liquid type intraurethral PGE 1 delivery formulation using a self-microemulsifying drug delivery system (i.e. SMEDDS). The liquid type intraurethral formulation has some pharmaceutical significances from the viewpoint of patients' compliance as follows; i) non-invasive drug delivery is possible, ii) administration is easier into the urethra than pellet type solid suppository products, and iii) less pain is expected.SMEDDS can be defined as an isotropic multi-component drug delivery system composed of surfactant, co-surfactant and oil, which in some cases transforms to viscous solution with contacting moisture and spontaneously forms microemulsion in the presence of excessive water.11-13) Traditionally, SMEDDS formulation has been used to increase dissolution rate or bioavailability of water insoluble drugs.14-16) The liquid type intraurethral formulation presented in this paper is practically a precursor mixture for forming a microemulsion. Thus, it is expected that the present SMEDDS formulation can be administered into the urethra by simple input procedure, reside in the urethra as a viscous liquid by taki...

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Section: Resultsmentioning

confidence: 99%

Design and Evaluation of Prostaglandin E1 (PGE1) Intraurethral Liquid Formulation Employing Self-Microemulsifying Drug Delivery System (SMEDDS) for Erectile Dysfunction Treatment

Lee

Choi

2008

Biological & Pharmaceutical Bulletin

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“…They show a resemblance to natural living tissues in terms of their water content and soft texture (15), while the high water content contributes to their biocompatibility. As a result, hydrogels are widely used as contact lenses membranes for biosensors, linings for artificial hearts, materials for artificial skin and drug delivery devices (15)(16)(17)(18)(19). Organogels are thermodynamically stable, viscoelastic bi-phasic systems comprising of a gelator and a organic phase, with or without the presence of water molecules within the network formed by the gelator _________________________________________ system.…”

Section: Gels In Drug Deliverymentioning

confidence: 99%

“…They are also known to be effective in moisturizing and revitalizing keratin-like tissues such as the hair, fingernails and skin. These gels consist of reversed polymer-like micelles, which evolve from spherical micelles seen initially, which agglomerate to form a temporal threedimensional network in the bulk phase and are obtained by the dissolution of trace amounts of water in a non-aqueous solution (19,38,42). Some in vivo studies have revealed the ability of PLO gels to be excellent drug carriers with penetration enhancement ability.…”

Section: Plo Gels For Transdermal Drug Deliverymentioning

confidence: 99%

Organogels in Drug Delivery: A Special Emphasis on Pluronic Lecithin Organogels

et al. 2016

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-Organogels have emerged as an alternative carrier for small and macromolecules via transdermal, oral, rectal and ophthalmic routes. Pluronic lecithin organogels (PLO gels) are lecithin-based organogels widely used in compounding pharmacies as a vehicle for enhancing the transdermal permeability of many therapeutic drugs. However, the scientific and systematic evidence in support of how well PLO gels help in transdermal delivery is scanty. Recently, some clinical studies have reported nearly complete lack of bioavailability of certain topically administered drugs from PLO gels. The present review aims at summarizing gels and organogels, with a focus on the use of PLO gels in transdermal drug delivery. A special emphasis is placed on controversies looming over the use of PLO gels as a delivery platform for drugs via transdermal route.

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“…12) Lecithin is not only biocompatible, it also promotes the percutaneous absorption of various drugs. [13][14][15][16][17] Reverse worms prepared using biocompatible oils in combination with lecithin and a polar substance permit the percutaneous absorption of preparations with minimal skin irritation. Such reverse worms can be used to deliver poorly soluble drugs composed of micellar structures.…”

mentioning

confidence: 99%

Skin Permeation of Testosterone from Viscoelastic Lecithin Reverse Wormlike Micellar Solution

Imai

Hashizaki

Yanagi

et al. 2016

Biological & Pharmaceutical Bulletin

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We evaluated testosterone-containing lecithin reverse wormlike micelles (reverse worms) composed of a polar substance/lecithin/isopropyl myristate for transdermal application. Water, D-ribose, or tetraglycerol were used as the polar substance and were key ingredients for forming the reverse worms. Using the reverse worms, 1 wt% of testosterone could be stably solubilized. When using D-ribose as polar substance, the maximum zero-shear viscosity of the reverse worms solution was higher than that of systems using water or tetraglycerol as the polar substance. The mechanism of skin permeation of testosterone from reverse worms solution was elucidated using skin permeation experiments with hairless mouse skin. When the structure of the reverse worms transitioned to lamellar liquid crystals at the skin/formulation interface, testosterone became supersaturated in the formulations. The structural transition occurred in systems using water or D-ribose as the polar substance, increasing the flux of testosterone. The flux of testosterone from reverse worms solution thus depends on the type of polar substance used.Key words reverse wormlike micelle; lecithin organogel; skin permeation; rheology; phase diagram; hairless mouse skin Recent advances in drug dosage forms have led to improved quality of life for patients. The transdermal dosage form, in particular, represents one of the most important drug delivery methods. Transdermal dosage forms enable avoidance of the hepatic first-pass effect, which can be problematic with oral administration. Another advantage of transdermal dosage forms is that they are easy to apply and remove from the skin. Based on these advantages, transdermal dosage forms have been adopted for a variety of medications.We investigated the possibility of using lecithin reverse wormlike micelle (called reverse worms) comprised of a polar substance/lecithin/oil as the vehicle for transdermal therapeutic application of testosterone (TES). Lecithin is an amphiphilic molecule composed of both hydrophilic and hydrophobic groups. In general, lecithin forms spherical or ellipsoidal reverse micelles when added alone to oil. When trace amounts of a polar substance (e.g., water) 1) are added to this solution, the polar substance can attach to the phosphate groups of the lecithin molecules via hydrogen bonding, widening the gap between the head groups of neighboring lecithin molecules. Thus, the value of the critical packing parameter decreases and the interface curvature of the molecular assembly subsequently induces the formation of reverse worms. As a result, phase transition from reverse spherical micelles to reverse worms takes place. These reverse worms become tangled in the oil and form a three-dimensional (3D) network throughout the solution, turning the solution into an gel-like solution (also called a lecithin organogel). [1][2][3][4][5][6] In this reverse micellar system the polar substance is the key ingredient for the formation of reverse worms. We have also identified other key ingredients that can be...

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Lecithin Organogel as Matrix for Transdermal Transport of Drugs

Cited by 147 publications

References 11 publications

Design and Evaluation of Prostaglandin E1 (PGE1) Intraurethral Liquid Formulation Employing Self-Microemulsifying Drug Delivery System (SMEDDS) for Erectile Dysfunction Treatment

Design and Evaluation of Prostaglandin E1 (PGE1) Intraurethral Liquid Formulation Employing Self-Microemulsifying Drug Delivery System (SMEDDS) for Erectile Dysfunction Treatment

Organogels in Drug Delivery: A Special Emphasis on Pluronic Lecithin Organogels

Skin Permeation of Testosterone from Viscoelastic Lecithin Reverse Wormlike Micellar Solution

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