Ionic Liquid-In-Oil Microemulsions Prepared with Biocompatible Choline Carboxylic Acids for Improving the Transdermal Delivery of a Sparingly Soluble Drug

Islam, Rafiqul; Chowdhury, Raihan; Wakabayashi, Rie; Kamiya, Noriho; Moniruzzaman, Muhammad; Goto, Masahiro

doi:10.3390/pharmaceutics12040392

Cited by 66 publications

(83 citation statements)

References 47 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Islam et al [ 47 ] developed a series of microemulsions with acyclovir and ionic liquid (choline oleate) to evaluate in vitro the permeation of acyclovir through the skin. The results obtained by those researchers revealed that the acyclovir permeation was intensified by using the ionic liquid.…”

Section: Discussionmentioning

confidence: 99%

Performance of Choline Geranate Deep Eutectic Solvent as Transdermal Permeation Enhancer: An In Vitro Skin Histological Study

et al. 2021

View full text Add to dashboard Cite

In the present research work, we addressed the changes in skin by which deep eutectic solvents (DES) enhanced transdermal permeation of bioactive compounds and propose a rationale for this mechanism. Several studies showed that these unusual liquids were ideal solvents for transdermal delivery of biomolecules, but to date, no histological studies relating the action of DES to changes in the structure of the outer skin barrier have been reported. In the research effort described herein, we presented an in-depth analysis of the changes induced in the skin by choline geranate DES, a compound with proven capabilities of enhancing transdermal permeation without deleterious impacts on the cells. The results obtained showed that a low percentage of DES acted as a transient disruptor of the skin structure, facilitating the passage of bioactive compounds dissolved in it.

show abstract

Section: Discussionmentioning

confidence: 99%

Performance of Choline Geranate Deep Eutectic Solvent as Transdermal Permeation Enhancer: An In Vitro Skin Histological Study

et al. 2021

View full text Add to dashboard Cite

show abstract

“…Several factors are involved in the penetration of the skin by DPS-2 carried within the oil core of the developed O/W microemulsion: (1) the low surface tension of the microemulsion, and, consequently, the close and prolonged contact with the skin, ensuring high concentration gradient for drug skin uptake; (2) the improved penetration of the microemulsion into the hair follicles, leading to improved delivery into viable skin layers (epidermis and/or dermis); (3) the perturbation of SC lipid matrix by interactions of the microemulsion’s components with the SC, leading to improved permeability through the SC lipid bilayers [ 59 ]. Actually, numerous studies have recently confirmed that, owing to relatively high surfactant concentration, microemulsions lead to alterations in skin barrier function, such as the disruption of intercellular regions of SC, due to the fluidization and/or extraction of the SC lipid matrix [ 61 , 62 , 63 ]. Dermal irritation is one of the most common adverse effects when applying formulations topically, therefore, when developing novel topical formulations, apart from efficacy, the assessment of the dermal irritation potential is a critical factor.…”

Section: Discussionmentioning

confidence: 99%

Biological Evaluation of Oil-in-Water Microemulsions as Carriers of Benzothiophene Analogues for Dermal Applications

et al. 2021

View full text Add to dashboard Cite

During the last decade, many studies have been reported on the design and formulation of novel drug delivery systems proposed for dermal or transdermal administration. The efforts focus on the development of biocompatible nanodispersions that can be delivered to the skin and treat severe skin disorders, including cancer. In this context, oil-in-water (O/W) microemulsions have been developed to encapsulate and deliver lipophilic bioactive molecules for dermal application. An O/W biocompatible microemulsion composed of PBS buffer, Tween 80, and triacetin was assessed for its efficacy as a drug carrier of DPS-2, a lead compound, initially designed in-house to inhibit BRAFV600E oncogenic kinase. The system was evaluated through both in vitro and ex vivo approaches. The cytotoxic effect, in the presence and absence of DPS-2, was examined through the thiazolyl blue tetrazolium bromide (MTT) cell proliferation assay using various cell lines. Further investigation through Western blotting revealed that cells died of necrosis. Porcine ear skin was used as a skin model to evaluate the degree of permeation of DPS-2 through skin and assess its retention. Through the ex vivo experiments, it was clarified that encapsulated DPS-2 was distributed within the full thickness of the stratum corneum (SC) and had a high affinity to hair follicles.

show abstract

“…Microemulsions are thermodynamically stable colloidal mixtures of two immiscible liquids (i.e., water and oil) stabilized by surfactant molecules [73]. ILs proved to be promising alternatives to these components, being able to replace oil, water, and surfactant phases (Figure 2), improving the delivery of APIs across biological membranes [74,75].…”

Section: Ils As Permeation Enhancers and Microemulsion Components For Drug Deliverymentioning

confidence: 99%

Ionic Liquids in Drug Delivery

et al. 2021

View full text Add to dashboard Cite

Ionic liquids (ILs) are molten salts composed of a large organic cation and an organic/inorganic anion. Due to their ionic character, most ILs present advantageous properties over conventional solvents, such as negligible volatility at atmospheric conditions and high thermal and chemical stabilities. The wide variety of IL anion–cation combinations allows these solvents to be designed to display a strong solvation ability for a myriad of active pharmaceutical ingredients (APIs) and (bio)polymers. Given these properties, ILs have been used as solvents and as formulation components in different areas of drug delivery, as well as novel liquid forms of APIs (API-ILs) applied in different stages of development of novel drug delivery systems. Furthermore, their combination with polymers and biopolymers has enabled the design of drug delivery systems for new therapeutic routes of administration.

show abstract

Ionic Liquid-In-Oil Microemulsions Prepared with Biocompatible Choline Carboxylic Acids for Improving the Transdermal Delivery of a Sparingly Soluble Drug

Cited by 66 publications

References 47 publications

Performance of Choline Geranate Deep Eutectic Solvent as Transdermal Permeation Enhancer: An In Vitro Skin Histological Study

Performance of Choline Geranate Deep Eutectic Solvent as Transdermal Permeation Enhancer: An In Vitro Skin Histological Study

Biological Evaluation of Oil-in-Water Microemulsions as Carriers of Benzothiophene Analogues for Dermal Applications

Ionic Liquids in Drug Delivery

Contact Info

Product

Resources

About