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Topical Photodynamic Therapy for Skin Diseases: Current Status of Preclinical and Clinical Research, Nanocarriers and Physical Methods for Photosensitizer Delivery
Published in Andreia Ascenso, Sandra Simões, Helena Ribeiro, Carrier-Mediated Dermal Delivery, 2017
Fabíola Silva Garcia Praça, Patricia Mazureki Campos, Josimar O. Eloy, Raquel Petrilli, Maria Vitória Lopes Badra Bentley, Wanessa Silva Garcia Medina
Liposomes are vesicles formed by bilayers of phospholipids that can accommodate hydrophilic and hydrophobic PSs. For example, lipophilic PSs such as phthalocyanine derivatives are solubilized into the bilayer region and hydrophilic PSs such as aminolevulinic acid solubilize in the inner core of liposomes [152]. Liposomes are regarded as versatile and superior compared to other lipid-based carriers, once they can have controllable sizes according to preparation procedures [158] as well as are able to decrease concentration of PSs and lower light doses [154]. Improvement of 5-ALA skin penetration from topical application using liposomes was reported in the last decade [149,159]. For example, liposomes containing lipid composition similar to mammalian stratum corneum such as ceramide type III, cholesterol, cholesteryl sulfate and palmitic acid, were able to promote effective PSs delivery into the skin [149]. However, malleable, flexible, and deformable liposomes such as ethosomes, flexosomes, and invasomes, respectively, are the new generation of liposomes developed for enhanced skin delivery (Fig. 4.5).
Essential Oils as Carrier Oils
Published in K. Hüsnü Can Başer, Gerhard Buchbauer, Handbook of Essential Oils, 2020
Romana Aichinger, Gerhard Buchbauer
The vehicle system in which the EO respectively the terpene will be carried also affects the penetration enhancement effect. Based on the physicochemical properties of the vehicles and their interaction with the SC, they cause a difference concerning the penetration. Some organic solvents like ethanol or propylene glycol even show a penetration-enhancing function and, hence, induce synergistic effects, but work as the formulation of the vehicle to dissolve the drug and the EO. Invasomes, which describe novel vesicles for transdermal drug delivery, consist of phospholipids, little amounts of ethanol, and terpene mixtures as enhancers. In comparison to liposomes or ethosomes, they cause a higher penetration rate. These vesicles are proved to possess the positive effects of both liposomes as potential carriers and terpenes as they are able to modify the skin barrier. Vehicles are needed because of the difficulties that occur while dissolving lipophilic EOs in water and the possible skin irritation when directly applying the EOs on the skin. Namely, the accumulation of the terpenes, when applied as pure EOs, is considerably higher than in vehicles, although proportionality to the penetrant concentration is not discovered. When not applied as pure EOs, there are a few possibilities of dermatological formulations like o/w emulsions, suspensions, oily solutions, hydrogels, ointments, or multi-layer transdermal patches. If grape seed oil is used as vehicle for EOs like linalool, linalyl acetate, terpinen-4-ol, citronellol, or α-pinene, the EOs are present completely dissolved compared to the o/w emulsion, where they are either dissolved in the oily internal phase or in micelles of surfactants or emulsified with the surfactants, forming an internal oily phase (Cal et al., 2005; Fung Chye Lim et al., 2009; Herman and Herman, 2014; Chen et al., 2016; Jiang et al., 2017).
Development of invaethosomes and invaflexosomes for dermal delivery of clotrimazole: optimization, characterization and antifungal activity
Published in Pharmaceutical Development and Technology, 2023
Sureewan Duangjit, Kozo Takayama, Sureewan Bumrungthai, Jongjan Mahadlek, Tanasait Ngawhirunpat, Praneet Opanasopit
The response surfaces indicated that an increase in ethanol resulted in an increase in skin permeation flux, whereas an increase in d-limonene resulted in a significant increase in the skin permeation flux of I-ETS (Figure 3(I)). The concentrations of ethanol and d-limonene were found to be directly related to the skin permeation of I-ETS. The d-limonene concentration (0.5–1.5%) predominantly enhanced the skin permeation of I-ETS more than the ethanol concentration (10–50%) in this study. The skin permeation flux of various drug-loaded invasomes (Narishetty and Panchagnula 2005; Dragicevic-Curic, Gräfe, et al. 2008; Dragicevic-Curic, Scheglmann, et al. 2008; Mura et al. 2013; El-Nabarawi et al. 2018; Ahmed and Badr-Eldin 2019) and ethosomes (Touitou et al. 2000; Chen et al. 2010; Maheshwari et al. 2012; Zaky 2016; Niu et al. 2019; Nair et al. 2021; Nair et al. 2022) was high. A subsequent increase in the skin permeation flux was clearly observed with a further increase in the d-limonene concentration by 1.5% in our study (Figure 3(I)).
Utilization of propranolol hydrochloride mucoadhesive invasomes as a locally acting contraceptive: in-vitro, ex-vivo, and in-vivo evaluation
Published in Drug Delivery, 2022
Mahmoud H. Teaima, Moaz A. Eltabeeb, Mohamed A. El-Nabarawi, Menna M. Abdellatif
Propranolol hydrochloride (PNL) loaded invasomes (INVs) were created by a thin film hydration approach by D-optimal design, after a screening experiment that illustrated the importance of different variables on INVs aspects. The optimum INV (INV14) contained 200 mg phospholipid, 1.5% cineole and 0.6% chitosan. The optimum INV was stable upon refrigeration for 3 months. Transmission electron microscopy displayed spherical INVs without aggregation. Ex-vivo studies concluded sustained effect, good vaginal deposition, and accumulation of PNL-loaded INV gel, compared to PNL gel, INVs, and PNL solution. Further, sperm motility assay proved the powerful inhibitory effect of INVs-gel. Histopathological studies demonstrated the safety of PNL-loaded INV gel for vaginal application to rats. Hence, it could be concluded that PNL-loaded INV gel could be considered a safe and effective formula that can be used to prolong the deposition of PNL within vaginal layers, to control birth, with minimized systemic side effects.
Optimized 2-methoxyestradiol invasomes fortified with apamin: a promising approach for suppression of A549 lung cancer cells
Published in Drug Delivery, 2022
Zuhier A. Awan, Shareefa A. AlGhamdi, Nabil A. Alhakamy, Solomon Z. Okbazghi, Mohamed A. Alfaleh, Shaimaa M. Badr-Eldin, Hibah M. Aldawsari, Mohammed A. S. Abourehab, Hani Z. Asfour, Shadi A. Zakai, Mohammad W. Alrabia, Aya A. Negm, Mohamed A. El-Moselhy, Sara S. Sharkawi, Waleed Y. Rizg
Invasomes (INVA) are innovative elastic vesicles made of several chemicals, including terpene(s), ethanol, and phosphatidylcholine (Ahmed & Badr-Eldin, 2019), which enhance the absorption of water soluble and lipid soluble drugs (Alhakamy et al., 2021). This enhancement can likely be attributed to terpenes, which break down the tightly packed lipids in epidermal (Ahmed & Badr-Eldin, 2019) and engage with intracellular proteins (Attalla et al., 1996). Similarly, ethanol helps the drugs seep through the stratum corneum. Moreover, it exhibits anti-angiogenic action through electrostatic repulsion by maintaining a negative surface charge (Ahmed & Badr-Eldin, 2019). INVA have shown promising activity against MCF-7 breast cancer cell line (Vidya & Lakshmi, 2019)