Evaluation of thiolated silicone oil as advanced mucoadhesive antifoaming agent

Abstract

Context: Silicone oils, such as dimethicone, are commonly administered against gastrointestinal gas accumulation and are attributed with mucoprotective features. Objective: Evaluation of thiolated silicone oil as advanced antiflatulence with a prolonged retention on small intestinal mucosa as an intended site of action. Materials and methods: 3-Mercaptopropionic acid (MPA) as a thiol ligand was covalently attached to silicone oil. This thiomer was assessed with regard to foam inhibiting action, droplet size of a suitable self-emulsifying system, mucoadhesion and cytotoxicity. Results: Antifoaming activity of silicone-MPA was complying with United States Pharmacopeia (USP) requirements for simethicone as standard antiflatulence. Another antifoaming test performed on porcine mucosa supported silicone-MPA's outstanding foam destruction, as this thiomer was superior in comparison to non-thiolated silicone oil and dimethicone with 14.7 ± 2.1 versus 73.3 ± 9.1 and 66.3 ± 7.5 s, respectively. A significantly enhanced mucoadhesiveness (p50.02) with 26.2 ± 7.1% silicone formulation remaining on small intestinal mucosa after 8 h was evident for the thiomer without any toxic effect. Conclusion: Thiolated silicone oil was found to exhibit excellent antifoaming and superior mucoadhesive features. The prolonged residence time of thiolated silicone oil promises to be beneficial in the treatment of flatulence, aerophagy and inflammation throughout the whole gastrointestinal tract.

Thiolated Silicone Oils as New Components of Protective Creams in the Prevention of Skin Diseases

“…The high viscosity of the oil phase made it difficult to break it down into smaller droplets. This is in good agreement with results published by Nazir et al [ 39 ], yet contrary to works by Partenhauser [ 40 ]. There, the self-emulsifying drug delivery system (containing stearic acid, Span 80 Bri O 10, butanol) obtained by the authors did not present statistically significant differences in the droplet size for systems containing amino silicone oils and silicone-MPA.…”

“…We used triethanolamine stearate with HLB 20 [ 41 ] and PEG-8 stearate with HLB 11.1 [ 42 ], which allowed us to obtain stable samples regardless of the silicon oil used. Long acid chains can stabilize the lipophilic silicone molecule inside the micelle due to hydrophobic interactions [ 40 ].…”

“…The adhesion of thiomers to mucous membranes, the indications of the presence of free thiol groups in human skin, and the versatile use of silicones in skin applications were the starting point for silicone-MPA and silicone-TGA research [ 8 , 17 , 18 ]. This research concerned both the determination of the characteristics affecting dermoadhesion for thiolated silicone oil derivatives [ 8 ] and an assessment of their potential as dermoadhesive excipients [ 18 ].…”

“…These new derivatives may interact with those disulfide bridges through interchanging reactions. A keratin-thiolated silicone oil network can be created, and the thiomers attach to the skin surface [ 8 , 17 , 18 , 20 ]. Another reason that thiolated silicone oils are adhesive is the fact that interactions between keratin layers, which are the major components in the stratum corneum as the outermost shield of the skin, can occur [ 8 , 18 ].…”

<p>Development and Characterization of A New Dimethicone Nanoemulsion and its Application for Electronic Gastroscopy Examination</p>

“…Figure 1 also shows that the strongest defoaming ability is neither high viscosity (1000 mPa.s) nor low viscosity DM (10 mPa.s and 50 mPa.s), but intermediate viscosity DM (350 mPa.s and 500 mPa.s), this consequence is inconsistent with the literature reports. 35,36 Many factors may affect the results of measuring the defoaming rate, among them, the method adopted and human operation are the main influencing elements, though the trend of the measurement results is consistent. 27,37 In order to choose a suitable oil phase, besides the viscosity and defoaming rate of DM, it is essential to consider the emulsification situation of DM with different viscosity in the mixture of emulsifier, co-emulsifier and water.…”