Solubility-physicochemical-thermodynamic theory of penetration enhancer mechanism of action

Haq, Anika; Chandler, Mark; Michniak‐Kohn, Bozena

doi:10.1016/j.ijpharm.2019.118920

Cited by 28 publications

(12 citation statements)

References 17 publications

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“…Generally, enhancers combining high potency and safety are believed to act on the intercellular stratum corneum lipids because these lipids provide the major permeation pathway for most drugs 10 . The mechanism of action of enhancers can be related to solubility parameters, physicochemical interactions, and thermodynamic activity as suggested by recently introduced solubility-physicochemicalthermodynamic theory 11 .…”

Section: Introductionmentioning

confidence: 99%

Effect of Essential Oils on Transdermal Permeation of Metoprolol Succinate

Sorathia

Patel

Soni

et al. 2021

Bulletin of Pharmaceutical Sciences. Assiut

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The objective of the present study was to prepare a matrix-type transdermal drug delivery system containing metoprolol succinate and to evaluate the effect of essential oils on transdermal permeation of drug. The solvent evaporation method was employed to fabricate transdermal patches of drug using HPMC K15M and Acrycoat L100 as polymers and polyethylene glycol 400 as a plasticizer. Prepared patches were subjected for evaluation of physical as well as physicochemical properties, moisture characteristics, and ex-vivo drug permeation studies. The results of physical characterization showed uniform casting and good appearance of patches. Satisfactory mechanical strength was revealed in the results of tensile strength and folding endurance. Ex-vivo permeation study indicated enhancing effect of essential oils on drug permeation through the skin. The maximum flux observed was 94 µg/cm2.hr achieved by formulation M3 containing lemongrass oil (20%). The results suggested that lemongrass oil was effective at higher concentration (20%) after 14 hrs of permeation while peppermint oil and eucalyptus oil were effective at low concentration (10%). Release kinetic suggested diffusion-controlled release of drug which followed the Korsmeyer-Peppas model. In conclusion, essential oils can be utilized as a safe and effective alternative for the permeation enhancement of drugs through transdermal delivery. Authors are thankful to Troikaa Pharmaceuticals Ltd., Ahmedabad for providing gift sample of Metoprolol succinate. Authors are also thankful to Shin-Etsu Chemical Co. Ltd., Japan and Corel Pharma Chem, Ahmedabad for providing Metolose (HPMC) and Acrycoat L100 as gift samples.

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Section: Introductionmentioning

confidence: 99%

Effect of Essential Oils on Transdermal Permeation of Metoprolol Succinate

Sorathia

Patel

Soni

et al. 2021

Bulletin of Pharmaceutical Sciences. Assiut

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“…CTAB is a cationic surfactant whose mechanism of action is linked to its ability of doing micelles with lipids from cellular membrane, which break the cellula (Cárdenas, 2016). As the efficacy of the most of penetration enhancers depends on their concentration (Haq et al, 2020), initially it is proposed that the used concentration of CTAB in this study was under the effective concentration for enhancing butorphanol penetration through equine nasal mucosa.…”

Section: Discussionmentioning

confidence: 98%

“…Most of substances cross biological membranes through diffusion, a phenomena which is described by Fick Law (Haq et al, 2020) assuming that the velocity of transference per unit area (flux) of a membrane is a direct function of its thickness (Talevi & Bellera, 2016, p 27), consequently is expected to butorphanol is more crossed through olfactory nasal mucosa than respiratory nasal mucosa, because the first is thinner than the second.…”

Section: Discussionmentioning

confidence: 99%

Effect of two surfactants on in vitro permeation of butorphanol through horse nasal mucosa

2021

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The aim of the present study was to evaluate the effect of two surfactants on in vitro permeation of butorphanol through equine nasal mucosa. Franz diffusion cells and equine nasal mucosa were used. Three formulations were developed based on citric acid, sodium citrate, sodium chloride, and butorphanol tartrate and administered at a 24.4 g cm-3 dose. Control formulation lacked any penetration enhancer. Formulation 1 (F1) had a cationic surfactant (cetrimonium bromide) and formulation 2 (F2) had a non-ionic surfactant (Tween 80). Statistically comparing flux values at the steady state (Jss), apparent permeability coefficient (Kp), and lag-time from control, F1 and F2 for the respiratory region does not show statistically significant differences (α= 0.05). However, statistically significant differences were found on the Jss and Kp, values from control, F1, and F2 in olfactory mucosa. A statistical analysis on the latter showed significant differences between the Jss values of F1 and F2 and between control and F2. Based on this, Tween 80 proved to be a promising excipient in developing intranasal butorphanol formulations in equines since it increases its passage through the nasal mucosa. These results are very promising to continue with the development of intranasal butorphanol formulation in equines.

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“…To use FFE, active ingredients and excipients are entered by using their Simplified Molecular Input Line Entry Specification (SMILES) code, and the software then generates their solubility and physicochemical properties. These properties include but are not limited to the ingredient active gap (IAG), active formulation gap (AFG), ingredient skin gap (ISG), molar volume (MVol), and Hansen solubility parameters (HSP; δD, δP, and δH values) [ 181 ]. FFE is only set up for optimizing lipophilic actives, yet it is still possible to run a simulation with a hydrophilic active.…”

Section: Formulating For Efficacy™ (Ffe)mentioning

confidence: 99%

Transdermal Delivery of Chemotherapeutics: Strategies, Requirements, and Opportunities

et al. 2021

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Chemotherapeutic drugs are primarily administered to cancer patients via oral or parenteral routes. The use of transdermal drug delivery could potentially be a better alternative to decrease the dose frequency and severity of adverse or toxic effects associated with oral or parenteral administration of chemotherapeutic drugs. The transdermal delivery of drugs has shown to be advantageous for the treatment of highly localized tumors in certain types of breast and skin cancers. In addition, the transdermal route can be used to deliver low-dose chemotherapeutics in a sustained manner. The transdermal route can also be utilized for vaccine design in cancer management, for example, vaccines against cervical cancer. However, the design of transdermal formulations may be challenging in terms of the conjugation chemistry of the molecules and the sustained and reproducible delivery of therapeutically efficacious doses. In this review, we discuss the nano-carrier systems, such as nanoparticles, liposomes, etc., used in recent literature to deliver chemotherapeutic agents. The advantages of transdermal route over oral and parenteral routes for popular chemotherapeutic drugs are summarized. Furthermore, we also discuss a possible in silico approach, Formulating for Efficacy™, to design transdermal formulations that would probably be economical, robust, and more efficacious.

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Solubility-physicochemical-thermodynamic theory of penetration enhancer mechanism of action

Cited by 28 publications

References 17 publications

Effect of Essential Oils on Transdermal Permeation of Metoprolol Succinate

Effect of Essential Oils on Transdermal Permeation of Metoprolol Succinate

Effect of two surfactants on in vitro permeation of butorphanol through horse nasal mucosa

Transdermal Delivery of Chemotherapeutics: Strategies, Requirements, and Opportunities

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