Journal ArticleDOI
Poloxamer 407/TPGS Mixed Micelles as Promising Carriers for Cyclosporine Ocular Delivery
Maria Aurora Grimaudo,Silvia Pescina,Cristina Padula,Patrizia Santi,Angel Concheiro,Carmen Alvarez-Lorenzo,Sara Nicoli +6 more
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TLDR
Developing an aqueous micellar formulation for an efficient cyclosporine delivery to the ocular tissues, using a water-soluble derivative of vitamin E and vitamin E succinate from TPGS and poloxamer 407 as excipients demonstrated the capability of mixed micelles to diffuse into the sclera and sustain cyclospora delivery.Abstract:
Cyclosporine is an immunosuppressant agent approved for the treatment of dry eye disease and used off-label for other ocular pathologies. Its formulation and ocular bioavailability present a real challenge due to the large molecular weight (1.2 kDa), high lipophilicity, and low water solubility. The aim of the work was to develop an aqueous micellar formulation for an efficient cyclosporine delivery to the ocular tissues, using a water-soluble derivative of vitamin E (TPGS: d-α-tocopheryl polyethylene glycol 1000 succinate) and poloxamer 407 (Pluronic ®F127) as excipients. The mixed micelles were characterized in terms of particle size, zeta potential, rheology, and stability upon dilution and freeze-drying. Additionally, the enzymatic-triggered release of vitamin E and vitamin E succinate from TPGS was investigated in vitro in the presence of esterase. Compared to the commercially available ophthalmic formulation, the poloxamer 407:TPGS 1:1 molar ratio micellar formulation significantly improved cyclospo...read more
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Soluplus micelles for acyclovir ocular delivery: Formulation and cornea and sclera permeability.
TL;DR: Test whether encapsulation of acyclovir in Soluplus or Solutol polymeric micelles increases its solubility, corneal permeability and sclera penetration, and the micelle formulation significantly shortened the permeation lag time through the cornea.
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Insights into the Dissolution Behavior of Ledipasvir-Copovidone Amorphous Solid Dispersions: Role of Drug Loading and Intermolecular Interactions.
Chailu Que,Xiaochun Lou,Dmitry Zemlyanov,Huaping Mo,Anura S. Indulkar,Yi Gao,Geoff G. Z. Zhang,Lynne S. Taylor +7 more
TL;DR: Evidence is provided that the extent of drug-polymer interactions as a function of DL play a central role in dictating the observed release behavior and a formulation strategy to increase the LoC.
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Solutol HS15 based binary mixed micelles with penetration enhancers for augmented corneal delivery of sertaconazole nitrate: optimization, in vitro, ex vivo and in vivo characterization.
TL;DR: The obtained results suggest that the aforementioned STZ loaded mixed micellar system could be an effective candidate for Keratomycosis-targeted therapy.
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PEO-PPO-PEO Tri-Block Copolymers for Gene Delivery Applications in Human Regenerative Medicine-An Overview.
Ana Rey-Rico,Magali Cucchiarini +1 more
TL;DR: The state of art of the application of PEO-PPO-PEO copolymers in both nonviral and viral gene transfer approaches and their potential as gene delivery systems in different regenerative medicine approaches are summarized.
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Topical application of polymeric nanomicelles in ophthalmology: a review on research efforts for the noninvasive delivery of ocular therapeutics.
Maria Aurora Grimaudo,Silvia Pescina,Cristina Padula,Patrizia Santi,Angel Concheiro,Carmen Alvarez-Lorenzo,Sara Nicoli +6 more
TL;DR: The aim of this review was to gather up-to-date information on the different roles that polymeric micelles (commonly in the nanosize scale) can play in ocular delivery, and focuses on those properties that are relevant for ophthalmic application.
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Vitamin E TPGS as a molecular biomaterial for drug delivery
TL;DR: TPGS has an amphiphilic structure of lipophilic alkyl tail and hydrophilic polar head with a relatively low critical micelle concentration (CMC) of 0.02% w/w, which make it to be an ideal molecular biomaterial in developing various drug delivery systems, including prodrugs, micelles, liposomes and nanoparticles.