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Essential Oils as Carrier Oils
Published in K. Hüsnü Can Başer, Gerhard Buchbauer, Handbook of Essential Oils, 2020
Romana Aichinger, Gerhard Buchbauer
For the in vitro permeation experiments, Franz-type diffusion cells can be used. Therefore, the prepared skin surface of about 1.7 cm2 is mounted between the donor and receptor chambers with the SC side facing the donor compartment. The donor compartment is filled with vehicle-containing drugs and penetration enhancers while the receptor phase consists of buffer pH 7.4, maintained at 37°C and stirred at about 500–600 rpm. To find out whether or not the penetration enhancer is helpful for the drug to overcome the SC barrier, the experiment is carried out with and without it, and the drug concentrations of the collected samples from the receptor compartments are compared (Fang et al., 2004; Brito et al., 2009; Feng et al., 2015; Jiang et al., 2017).
Development of Topical and Transdermal Dosage Forms
Published in Tapash K. Ghosh, Dermal Drug Delivery, 2020
The chemical penetration enhancers have functional characteristics of increasing skin permeation rate; therefore, they are controlled by ID, assay, purity, melting point, etc. On rare occasions, novel penetration enhancers are used. The novel penetration enhancers are treated in a manner similar to that of a new molecular entity. Therefore, complete characterization and toxicity information may be required. Applicants are recommended to contact the respective clinical divisions for the specific requirements for the novel penetration enhancers. Compendial chemical penetration enhancers are most common since once a pharmaceutical use of the penetration enhancer is identified by the manufacturer of the penetration enhancer, the company facilitates the compendial monograph process for this specific chemical.
Development of Ethosome Formulation for Topical Therapeutic Applications
Published in Madhu Gupta, Durgesh Nandini Chauhan, Vikas Sharma, Nagendra Singh Chauhan, Novel Drug Delivery Systems for Phytoconstituents, 2020
Mansoureh Nazari Vishkaei, Mohamed B. Khadeer Ahamed, Amin Malik Shah Abdul Majid
Penetration enhancer-containing vesicles have been researched thoroughly and ultimately introduced and developed a novel category of extremely improved cutaneous delivery of minoxidil. The formulation primarily contained penetration enhancers. Some soya lecithin, ethanol, and cineole are penetration enhancers. The results showed that such enhancers could provide statistically significant development in deposition of minoxidil through skin layers compared with typical liposomes as well as penetration enhancers in specific hydroethanolic solution. Additionally, the foremost flexible penetration enhancers, optimized with cineole, were extremely effective within the delivery of minoxidil within the skin, suggesting that delivery of minoxidil after topical application may correlate with the deforming of vesicles and, therefore, successively relate to vesicle composition (Manconi et al., 2011). These systems represent a proper combination of liposomal ability in order to be used as carrier and penetration interest that is able to penetrate deeply into stratum corneum cellular arrangement, so promoting the skin penetrance and thence the drug delivery.
Insightful exploring of advanced nanocarriers for the topical/transdermal treatment of skin diseases
Published in Pharmaceutical Development and Technology, 2021
Ghada M. El-Zaafarany, Maha Nasr
PEVs are a type of deformable vesicles in which hydrophilic penetration enhancers are incorporated into the phospholipid bilayer (Figure 6) to impart membrane fluidity (Mura et al. 2009; Barakat et al. 2017), with the type of enhancer having a major effect on the performance of the vesicles. Amongst such penetration enhancers, the most commonly used are propylene glycol, transcutol, and labrasol (Manconi et al. 2011), as well as, limonene and oleic acid (El Maghraby et al. 2004). Hence, PEVs exhibit the combinatorial advantages of liposomes as carriers, as well as, transient reduction of the SC barrier function and improvement in vesicular bilayer fluidity due to the incorporated penetration enhancer (Bsieso et al. 2015; Roberts et al. 2017). Some of the applications of PEVs in dermal skin delivery are represented in Table 8.
Emulgel: an effective drug delivery system
Published in Drug Development and Industrial Pharmacy, 2021
Maria Talat, Muhammad Zaman, Rahima Khan, Muhammad Jamshaid, Muneeba Akhtar, Agha Zeeeshan Mirza
Properties of penetration enhancer. Following are the few properties that should be considered before using a penetration enhancer for the preparation of emulgel.They ought not to have any pharmacological action inside the body. It implies that they ought not to tie to any of the receptor sites [20].They ought to be worthy cosmetically with skin and should not cause any kind of skin irritation or disturbance [12].Properties like non-toxicity, less irritability, and non-unfavorably susceptibility should be present [23].They ought to show favorable compatibility with the drugs and the excipients added [44].When it is removed from the skin, barrier properties should return rapidly [35].
Development of rebamipide-loaded spray-dried microsphere using distilled water and meglumine: physicochemical characterization and pharmacokinetics in rats
Published in Pharmaceutical Development and Technology, 2021
Dae Woong Ko, Jung Hyun Cho, Han-Gon Choi
Rebamipide [2-(4-chlorobenzoylamino)-3-[2(1H)-quinolinon-4-yl] propionic acid], an amino acid derivative of 2-(1H)-quinolinone, has been used as a potent antiulcer agent, because it increases endogenous prostaglandin synthesis and scavenges oxygen-derived free radicals in damaged gastric mucosal cells (Holland et al. 2019; Jaafar et al. 2018; Simsek et al. 2019). It is a BCS (Biopharmaceutics Classification System) class IV drug, because of its low solubility and permeability (Ha et al. 2017; Takeuchi et al. 2018). In particular, rebamipide has been reported to provide absolute oral bioavailability of 4.8% in rats (Shi et al. 2013). Therefore, the solubility and permeability of oral rebamipide in the gastrointestinal tract are two factors in its enhanced oral bioavailability. Much research has been focused on its enhanced bioavailability resulting from increased permeability with penetration enhancers (Huang et al. 2008; Mustapha, Din, et al. 2016; Narala et al. 2019; Tanaka et al. 2019). However, the use of specific penetration enhancers has not been approved by the US FDA since these materials might induce severe irritation to biological membranes. Many solubility-enhancing techniques, such as solid dispersion (Pradhan et al. 2015; Xiong et al. 2017; Takeuchi et al. 2018; Tanaka et al. 2019), nanosuspension (Shi et al. 2013), orally disintegrating tablets (Takano et al. 2019) and nano/microemulsion (Kim et al. 2017; Narala et al. 2019), have been studied.