“…Solutol ® HS-15 (HS15), a nonionic surfactant, comprised of 70% of polyglycol mono- and di-esters of 12-hydroxystearic acid and 30% of free polyethylene glycol (Hou et al, 2016 ). It is characterized by its high stability, good biocompatibility, enhanced mucosal permeability, excellent solubilization power of hydrophobic drugs, and the ability to alter the pharmacokinetics of many drugs (Alani et al., 2010 ; Shubber et al., 2015 ). The past few years have witnessed the use of HS15 in the development of several ocular drug delivery systems, these systems were investigated and found to have promising outcomes regarding either corneal permeability or corneal retention (Gan et al., 2009 ; Chen et al., 2013 ).…”
Keratomycosis is a serious corneal disease that can cause a permanent visual disability if not treated effectively. Sertaconazole nitrate (STZ), a novel broad spectrum antifungal drug, was suggested as a promising treatment. However, its utility in the ocular route is restricted by its poor solubility, along with other problems facing the ocular delivery like short residence time, and the existing corneal barrier. Therefore, the objective of this study was to formulate STZ loaded binary mixed micelles (STZ-MMs) enriched with different penetration enhancers using thin-film hydration method, based on a 31.22 mixed factorial design. Different formulation variables were examined, namely, type of auxiliary surfactant, type of penetration enhancer, and total surfactants: drug ratio, and their effects on the solubility of STZ in MMs (SM), particle size (PS), polydispersity index (PDI), and zeta potential (ZP) were evaluated. STZ-MMs enhanced STZ aqueous solubility up to 338.82-fold compared to free STZ. Two optimized formulations (MM-8 and MM-11) based on the desirability factor (0.891 and 0.866) were selected by Design expert® software for further investigations. The optimized formulations were imaged by TEM which revealed nanosized spherical micelles. Moreover, they were examined for corneal mucoadhesion, stability upon dilution, storage effect, and ex vivo corneal permeation studies. Finally, both in vivo corneal uptake and in vivo corneal tolerance were investigated. MM-8 showed superiority in the ex vivo and in vivo permeation studies when compared to the STZ-suspension. The obtained results suggest that the aforementioned STZ loaded mixed micellar system could be an effective candidate for Keratomycosis-targeted therapy.
“…Solutol ® HS-15 (HS15), a nonionic surfactant, comprised of 70% of polyglycol mono- and di-esters of 12-hydroxystearic acid and 30% of free polyethylene glycol (Hou et al, 2016 ). It is characterized by its high stability, good biocompatibility, enhanced mucosal permeability, excellent solubilization power of hydrophobic drugs, and the ability to alter the pharmacokinetics of many drugs (Alani et al., 2010 ; Shubber et al., 2015 ). The past few years have witnessed the use of HS15 in the development of several ocular drug delivery systems, these systems were investigated and found to have promising outcomes regarding either corneal permeability or corneal retention (Gan et al., 2009 ; Chen et al., 2013 ).…”
Keratomycosis is a serious corneal disease that can cause a permanent visual disability if not treated effectively. Sertaconazole nitrate (STZ), a novel broad spectrum antifungal drug, was suggested as a promising treatment. However, its utility in the ocular route is restricted by its poor solubility, along with other problems facing the ocular delivery like short residence time, and the existing corneal barrier. Therefore, the objective of this study was to formulate STZ loaded binary mixed micelles (STZ-MMs) enriched with different penetration enhancers using thin-film hydration method, based on a 31.22 mixed factorial design. Different formulation variables were examined, namely, type of auxiliary surfactant, type of penetration enhancer, and total surfactants: drug ratio, and their effects on the solubility of STZ in MMs (SM), particle size (PS), polydispersity index (PDI), and zeta potential (ZP) were evaluated. STZ-MMs enhanced STZ aqueous solubility up to 338.82-fold compared to free STZ. Two optimized formulations (MM-8 and MM-11) based on the desirability factor (0.891 and 0.866) were selected by Design expert® software for further investigations. The optimized formulations were imaged by TEM which revealed nanosized spherical micelles. Moreover, they were examined for corneal mucoadhesion, stability upon dilution, storage effect, and ex vivo corneal permeation studies. Finally, both in vivo corneal uptake and in vivo corneal tolerance were investigated. MM-8 showed superiority in the ex vivo and in vivo permeation studies when compared to the STZ-suspension. The obtained results suggest that the aforementioned STZ loaded mixed micellar system could be an effective candidate for Keratomycosis-targeted therapy.
“…Co-surfactants are usually more hydrophilic; therefore, they act as emulsifying, solubilizing, and wetting agents as they have generally a higher HLB value from 12 to 16 and a higher molecular weight of over 1000 Da. Co-surfactants are commonly used in the literature for niosome formulations, for example Cremophor ® ELP (purified polyoxyl 35 castor oil) [17], Cremophor ® RH40 (hydrogenated polyoxyl 40 castor oil) [18], and Solutol ® HS15 (polyoxyl 15 hydroxystearate) [19]. Solutol ® HS15 is known to inhibit P-glycoprotein, which is an ATP-dependent pump that is responsible for reducing drug intestinal absorption by efflux transportation.…”
Novel niosomal formulations containing cinnarizine were developed to enhance its drug characteristics. In this work, niosomes (non-ionic surfactant vesicles) were prepared by conventional thin-film hydration (TFH) and microfluidic (MF) methods with sorbitan monostearate (Span® 60), cholesterol, and co-surfactants (Cremophor® ELP, Cremophor® RH40 and Solutol® HS15) as key excipients. The aim was to study the effect of cinnarizine on the characteristics of different niosomal formulations manufactured by using different methods. For effective targeted oral drug delivery, the efficacy of niosomes for therapeutic applications is correlated to their physiochemical properties. Niosome vesicles prepared were characterised using dynamic light scattering technique and the morphology of niosomes dispersion was characterised using optical microscopy. Dialysis was carried out to purify niosome suspensions to determine drug loading and drug release studies was performed to study the potential use of niosomal systems for cinnarizine.
“…CriticalSorb® technology is currently in early clinical development stage as a nasal spray formulation for delivery of human growth hormone, based on a previously demonstrated enhancement of the bioavailability of human growth hormone and insulin in both animal studies and human trials ( 8 ). In addition, Solutol® HS15 is currently used to increase the aqueous solubility of Biopharmaceutical Classification System (BCS) Class 2 and 4 lipophilic molecules ( 9 ). Fig.…”
PurposeCriticalSorb™, with the principal component Solutol® HS15, is a novel mucosal drug delivery system demonstrated to improve the bioavailability of selected biotherapeutics. The intention of this study is to elucidate mechanism(s) responsible for the enhancement of trans-mucosal absorption of biological drugs by Solutol® HS15.MethodsMicelle size and CMC of Solutol® HS15 were determined in biologically relevant media. Polarised airway Calu-3 cell layers were used to measure the permeability of a panel of biological drugs, and to assess changes in TEER, tight junction and F-actin morphology. The rate of cell endocytosis was measured in vitro in the presence of Solutol® HS15 using a membrane probe, FM 2–10.ResultsThis work initially confirms surfactant-like behaviour of Solutol® HS15 in aqueous media, while subsequent experiments demonstrate that the effect of Solutol® HS15 on epithelial tight junctions is different from a ‘classical’ tight junction opening agent and illustrate the effect of Solutol® HS15 on the cell membrane (endocytosis rate) and F-actin cytoskeleton.ConclusionSolutol® HS15 is the principle component of CriticalSorb™ that has shown an enhancement in permeability of medium sized biological drugs across epithelia. This study suggests that its mechanism of action arises primarily from effects on the cell membrane and consequent impacts on the cell cytoskeleton in terms of actin organisation and tight junction opening.
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