Mechanism of Mucosal Permeability Enhancement of CriticalSorb® (Solutol® HS15) Investigated In Vitro in Cell Cultures

Shubber, Saif; Vllasaliu, Driton; Rauch, Cyril; Jordan, Faron; Illum, Lisbeth; Stolnik, Snow

doi:10.1007/s11095-014-1481-5

Cited by 52 publications

(29 citation statements)

References 38 publications

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“…Soluplus ® is a hydrophilic graft copolymer, which can easily form colloidal micelles with very good solubilization ability and stability, due to its low value of CMC (0.76 × 10 −3 %, 0.0003 mM) [ 53 , 54 ]. Solutol ® HS15 has a CMC of 0.005–0.02% (0.06 mM in distilled water) [ 55 ]. Thanks to its unique solubilization characteristics and safety profiles, this excipient has been used in parenteral, oral, ophthalmic, macromolecule, and protein formulations.…”

Section: Resultsmentioning

confidence: 99%

Thymoquinone-Loaded Soluplus®-Solutol® HS15 Mixed Micelles: Preparation, In Vitro Characterization, and Effect on the SH-SY5Y Cell Migration

Bergonzi

Vasarri²,

Marroncini

et al. 2020

Molecules

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Thymoquinone (TQ) is the main active ingredient of Nigella sativa essential oil, with remarkable anti-neoplastic activities with anti-invasive and anti-migratory abilities on a variety of cancer cell lines. However, its poor water solubility, high instability in aqueous solution and pharmacokinetic drawbacks limits its use in therapy. Soluplus® and Solutol® HS15 were employed as amphiphilic polymers for developing polymeric micelles (SSM). Chemical and physical characterization studies of micelles are reported, in terms of size, homogeneity, zeta potential, critical micelle concentration (CMC), cloud point, encapsulation efficiency (EE%), load capacity (DL), in vitro release, and stability. This study reports for the first time the anti-migratory activity of TQ and TQ loaded in SSM (TQ-SSM) in the SH-SY5Y human neuroblastoma cell line. The inhibitory effect was assessed by the wound-healing assay and compared with that of the unformulated TQ. The optimal TQ-SSM were provided with small size (56.71 ± 1.41 nm) and spherical shape at ratio of 1:4 (Soluplus:Solutol HS15), thus increasing the solubility of about 10-fold in water. The entrapment efficiency and drug loading were 92.4 ± 1.6% and 4.68 ± 0.12, respectively, and the colloidal dispersion are stable during storage for a period of 40 days. The TQ-SSM were also lyophilized to obtain a more workable product and with increased stability. In vitro release study indicated a prolonged release of TQ. In conclusion, the formulation of TQ into SSM allows a bio-enhancement of TQ anti-migration activity, suggesting that TQ-SSM is a better candidate than unformulated TQ to inhibit human SH-SY5Y neuroblastoma cell migration.

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Section: Resultsmentioning

confidence: 99%

Thymoquinone-Loaded Soluplus®-Solutol® HS15 Mixed Micelles: Preparation, In Vitro Characterization, and Effect on the SH-SY5Y Cell Migration

Bergonzi

Vasarri²,

Marroncini

et al. 2020

Molecules

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“…Solutol HS-15, a non-ionic surfactant was reported to increase the permeability by disrupting the membrane structure and/or increasing the membrane fluidity [25] . Peltier et al also proved that Solutol HS-15 increased the plasma exposure of paclitaxel by inhibition of P-gp [26] . Paromomycin prepared with different combinations of excipients either P-gp inhibitors and membrane disruptors or both, showed increase in the oral bioavailability compared to CMC formulation.…”

Section: Table 3: Pharmacokinetic Parameters Of Paromomycin After IV mentioning

confidence: 95%

Investigation of Different Formulation Approaches to Enhance Oral Bioavailability of Paromomycin

Pinjari¹,

Somani²,

Gilhotra³

2017

pharmaceutical-sciences

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Pinjari, et al.: Different Formulation Approach for ParomomycinParomomycin, an aminoglycoside antibiotic, is used to treat visceral leishmaniasis as an intramuscular injection daily for 21 days since it has limited oral bioavailability. The objective of this investigation is to improve the oral bioavailability through formulation development for increased patient compliance and convenience. Comparative pharmacokinetic studies of intravenous and oral administration of paromomycin in mice to evaluate different formulation approaches to increase oral bioavailability were carried out. Following intravenous injection of 15 mg/kg to mice, paromomycin exhibited low plasma clearance (8 ml/min/kg) with elimination half-life of 2.6 h. Following oral administration of 500 mg/kg of a suspension formulation using carboxymethylcellulose to mice, referred to as formulation 1, paromomycin showed very low or negligible oral bioavailability (%F=0.3). Different formulation approaches were made by employing a variety of FDA-approved novel excipients belonging to glycols, fatty acids, alcohols and surfactants alone and in various combinations. In vivo pharmacokinetic studies with these formulations demonstrated improved oral bioavailability of paromomycin in mice. Formulation approaches tested in the present research project were successful in improving the oral bioavailability of paromomycin from 0.3% to a maximum of 9%. Overall, the increase in paromomycin bioavailability ranged 1-30 fold with different formulations compared to carboxymethylcellulose formulation. Formulation with 10% Gelucire 44/14, 10% Solutol HS 15, 30% propylene glycol and 50% normal saline showed higher bioavailability compared to formulation 1. This research provided evidence that improved bioavailability of paromomycin can be achieved through formulation development, which eventually could result in making the most tedious and painful intramuscular therapy redundant.

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“…For example, polyethylene glycol (15)-hydroxystearate or Kolliphor Ò HS 15 is a constituent of TA-LF; this reagent is a potent nonionic solubilizer and emulsifying agent with low toxicity proposed to act as a permeability enhancer that would promote drug transport across cell membranes (increasing the endocytosis rate) and improve drug translocation throughout the paracellular route (it affects actin organization in the cell cytoskeleton with subsequent tight junction opening). 35 Unfortunately, only a few reports have explored the relationship between CS outcomes and the use of antiinflammatory ophthalmic formulations in patients with PCME. For example, Ginsburg et al, reported in 1995 that patients who underwent manual extracapsular extraction improved their CS scores using ophthalmic formulations of flurbiprofen 0.03% or indomethacin 1%.…”

Section: Triamcinolone Acetonide-loaded Liposomes After Flacsmentioning

confidence: 99%

Novel Triamcinolone Acetonide-Loaded Liposomal Topical Formulation Improves Contrast Sensitivity Outcome After Femtosecond Laser-Assisted Cataract Surgery

Rosa

Navarro-Partida

Altamirano-Vallejo

et al. 2019

Journal of Ocular Pharmacology and Therapeutics

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Purpose: To assess visual results, macular modifications, and the incidence of clinically significant macular edema (CSME) in patients using a topical triamcinolone acetonide-loaded liposomal formulation (TA-LF) after femtosecond laser-assisted cataract surgery (FLACS). Methods: Fifty-six eyes after FLACS were selected. Twenty-eight eyes in the combined therapy group (P + N) were treated with prednisolone 1% and nepafenac 0.1% for 21 days postoperatively, whereas 28 eyes in the TA-LF group received a liposomal formulation containing 2 mg/mL of TA (0.2%) for the same period of time. Follow-up visits at 1 day, 6 weeks, and 12 weeks after surgery consisted of visual acuity, contrast sensitivity (CS), central foveal thickness (CFT), total macular volume (TMV) measurements, and the detection of CSME. Results: CS improved in the TA-LF group (basal value: 1.087-0.339 vs. 1.276-0.147 at week 12, P = 0.0346), whereas in the P + N group, CS was not different from the baseline (basal value: 1.130-0.331 vs. 1.274-0.133 at week 12, P = 0.1276). There were similar increases in postoperative CFT and TMV in both groups. CFT and TMV significantly correlate with CS only in the TA-LF group. The r 2 for CFT and CS was 0.1963 (P = 0.0206), whereas the r 2 for TMV and CS was 0.3615 (P = 0.0007) at 12 weeks. No difference was observed in the incidence of CSME between the groups. Conclusion: TA-LF is associated with better CS outcomes compared to combined therapy after FLACS.

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Mechanism of Mucosal Permeability Enhancement of CriticalSorb® (Solutol® HS15) Investigated In Vitro in Cell Cultures

Cited by 52 publications

References 38 publications

Thymoquinone-Loaded Soluplus®-Solutol® HS15 Mixed Micelles: Preparation, In Vitro Characterization, and Effect on the SH-SY5Y Cell Migration

Thymoquinone-Loaded Soluplus®-Solutol® HS15 Mixed Micelles: Preparation, In Vitro Characterization, and Effect on the SH-SY5Y Cell Migration

Investigation of Different Formulation Approaches to Enhance Oral Bioavailability of Paromomycin

Novel Triamcinolone Acetonide-Loaded Liposomal Topical Formulation Improves Contrast Sensitivity Outcome After Femtosecond Laser-Assisted Cataract Surgery

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