Drug Delivery Systems Based on Pluronic Micelles with Antimicrobial Activity

Abstract

Bacterial oral diseases are chronic, and, therefore, require appropriate treatment, which involves various forms of administration and dosing of the drug. However, multimicrobial resistance is an increasing issue, which affects the global health system. In the present study, a commercial amphiphilic copolymer, Pluronic F127, was used for the encapsulation of 1-(5′-nitrobenzimidazole-2′-yl-sulphonyl-acetyl)-4-aryl-thiosemicarbazide, which is an original active pharmaceutical ingredient (API) previously synthesized and characterized by our group, at different copolymer/API weight ratios. The obtained micellar systems, with sizes around 20 nm, were stable during 30 days of storage at 4 °C, without a major increase of the Z-average sizes. As expected, the drug encapsulation and loading efficiencies varied with the copolymer/API ratio, the highest values of 84.8 and 11.1%, respectively being determined for the F127/API = 10/1 ratio. Moreover, in vitro biological tests have demonstrated that the obtained polymeric micelles (PMs) are both hemocompatible and cytocompatible. Furthermore, enhanced inhibition zones of 36 and 20 mm were observed for the sample F127/API = 2/1 against S. aureus and E. coli, respectively. Based on these encouraging results, it can be admitted that these micellar systems can be an efficient alternative for the treatment of bacterial oral diseases, being suitable either by injection or by a topical administration.

Temperature Induced Gelation and Antimicrobial Properties of Pluronic F127 Based Systems

“…Thermosensitive Pluronic F127 is a desirable biomaterial for many applications in regenerative medicine or dentistry [ 1 , 2 , 3 , 4 , 5 , 6 , 7 , 8 ]. By itself, this copolymer does not show antimicrobial activity and the observations from the present study (sample 0) confirm this hypothesis.…”

“…Last decades, stimuli-responsive polymers were extensively investigated due to their high potential for many applications. Among them, the self-assembling of amphiphilic block copolymers into micelles and the temperature-induced gelation present a high interest in biomedical and pharmaceutical applications, as carriers for drug delivery [ 1 , 2 , 3 ], in regenerative medicine or dentistry [ 4 , 5 , 6 ], for preparing injectable hydrogels [ 7 ], in bioprinting [ 8 ], as sacrificial molding agents [ 9 ] etc. On the other hand, the proteins and renewable polysaccharides are non-toxic and endow some biological performances to biomaterials, such as biodegradability, biocompatibility, and mucoadhesive behavior.…”

“…The Pluronic-based gels present good printing properties and shape fidelity in physiological conditions, but they have modest cell viability [ 8 ] and structural integrity [ 17 , 18 ]. Some properties were improved in composites of PL with other synthetic polymers, such as poly(vinyl alcohol) [ 19 ], poly(aspartic acid) [ 20 ], poly(ethylene glycol) [ 21 ], or pharmaceutical ingredients [ 3 ]. The use of materials that combine the properties of PL with those of biomolecules is of high interest for bio-applications [ 15 , 22 , 23 , 24 , 25 ].…”

Development of pH-Responsive N-benzyl-N-O-succinyl Chitosan Micelles Loaded with a Curcumin Analog (Cyqualone) for Treatment of Colon Cancer

“…Loading of some synthetic hydrophobic compounds with polymeric micelles have been observed, with a predominant increase in their pharmacological profile [ 38 ]. In the current study, the curcumin analog was successfully loaded into NBSCh micelles via hydrophobic–hydrophobic interactions between the cyqualone and hydrophobic core of the NBSCh micelles.…”

Amphiphilic Block Copolymers: Their Structures, and Self-Assembly to Polymeric Micelles and Polymersomes as Drug Delivery Vehicles

“…Guiraud et al promoted 25R2 for DNA transfection of skeletal muscle in a similar manner to P105 [ 136 ]. Zhang et al reported the P123 and F127 mixed system for the treatment of multidrug-resistant tumors [ 137 ]. Hassanzadeh et al synthesized F127 and 10R5 mixed micelles for doxorubicin to enhance its therapeutic function and reduce the side effects to normal cells [ 138 ].…”