Poloxamer 407/TPGS Mixed Micelles as Promising Carriers for Cyclosporine Ocular Delivery

2018 ◽  
Vol 15 (2) ◽  
pp. 571-584 ◽  
Author(s):  
Maria A. Grimaudo ◽  
Silvia Pescina ◽  
Cristina Padula ◽  
Patrizia Santi ◽  
Angel Concheiro ◽  
...  
Keyword(s):  
Mixed Micelles ◽  
Poloxamer 407 ◽  
Ocular Delivery

scholarly journals Clozapine-Encapsulated Binary Mixed Micelles in Thermosensitive Sol–Gels for Intranasal Administration

Gels ◽  
2022 ◽  
Vol 8 (1) ◽  
pp. 38
Author(s):  
Madeleine S. A. Tan ◽  
Preeti Pandey ◽  
James R. Falconer ◽  
Dan J. Siskind ◽  
Alexandra Balmanno ◽  
...  
Keyword(s):  
Intranasal Administration ◽  
Mixed Micelles ◽  
Hydroxypropyl Methylcellulose ◽  
Particle Diameter ◽  
Poloxamer 407 ◽  
Carrier System ◽  
Drug Deposition ◽  
Polysorbate 20 ◽  
Release Studies ◽  
Amorphous Drug

(1) Background: Clozapine is the most effective antipsychotic. It is, however, associated with many adverse drug reactions. Nose-to-brain (N2B) delivery offers a promising approach. This study aims to develop clozapine-encapsulated thermosensitive sol–gels for N2B delivery. (2) Methods: Poloxamer 407 and hydroxypropyl methylcellulose were mixed and hydrated with water. Glycerin and carbopol solutions were added to the mixture and stirred overnight at 2–8 °C. Clozapine 0.1% w/w was stirred with polysorbate 20 (PS20) or polysorbate 80 (PS80) at RT (25 °C) before being added to the polymer solution. The final formulation was made to 10 g with water, stirred overnight at 2–8 °C and then adjusted to pH 5.5. (3) Results: Formulations F3 (3% PS20) and F4 (3% PS80) were selected for further evaluation, as their gelation temperatures were near 28 °C. The hydrodynamic particle diameter of clozapine was 18.7 ± 0.2 nm in F3 and 20.0 ± 0.4 nm in F4. The results show a crystallinity change in clozapine to amorphous. Drug release studies showed a 59.1 ± 3.0% (F3) and 53.1 ± 2.7% (F4) clozapine release after 72 h. Clozapine permeated after 8 h was 20.8 ± 3.0% (F3) and 17.8 ± 3.1% (F4). The drug deposition was higher with F4 (144.8 ± 1.4 µg/g) than F3 (110.7 ± 2.7 µg/g). Both sol–gels showed no phase separation after 3 months. (4) Conclusions: Binary PS80-P407 mixed micelles were more thermodynamically stable and rigid due to the higher synergism of both surfactants. However, binary mixed PS20-P407 micelles showed better drug permeation across the nasal mucosa tissue and may be a preferable carrier system for the intranasal administration of clozapine.

scholarly journals Ex Vivo Conjunctival Retention and Transconjunctival Transport of Poorly Soluble Drugs Using Polymeric Micelles

Pharmaceutics ◽  
2019 ◽  
Vol 11 (9) ◽  
pp. 476 ◽  
Author(s):  
Pescina ◽  
Lucca ◽  
Govoni ◽  
Padula ◽  
Favero ◽  
...  
Keyword(s):  
Polymeric Micelles ◽  
Ex Vivo ◽  
Water Soluble ◽  
Poloxamer 407 ◽  
Conjunctival Epithelium ◽  
Ocular Delivery ◽  
Lipophilic Drugs ◽  
Polyethylene Glycol 1000 ◽  
The One

This paper addresses the problem of ocular delivery of lipophilic drugs. The aim of the paper is the evaluation of polymeric micelles, prepared using TPGS (d-α-Tocopheryl polyethylene glycol 1000 succinate), a water-soluble derivative of Vitamin E and/or poloxamer 407, as a vehicle for the ocular delivery of dexamethasone, cyclosporine, and econazole nitrate. The research steps were: (1) characterize polymeric micelles by dynamic light scattering (DLS) and X-ray scattering; (2) evaluate the solubility increase of the three drugs; (3) measure the in vitro transport and conjunctiva retention, in comparison to conventional vehicles; (4) investigate the mechanisms of enhancement, by studying drug release from the micelles and transconjunctival permeation of TPGS; and (5) study the effect of micelles application on the histology of conjunctiva. The data obtained demonstrate the application potential of polymeric micelles in ocular delivery, due to their ability to increase the solubility of lipophilic drugs and enhance transport in and across the conjunctival epithelium. The best-performing formulation was the one made of TPGS alone (micelles size ≈ 12 nm), probably because of the higher mobility of these micelles, an enhanced interaction with the conjunctival epithelium, and, possibly, the penetration of intact micelles.

scholarly journals Preliminary Investigation on Simvastatin-Loaded Polymeric Micelles in View of the Treatment of the Back of the Eye

Pharmaceutics ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 855
Author(s):  
Silvia Pescina ◽  
Fabio Sonvico ◽  
Adryana Clementino ◽  
Cristina Padula ◽  
Patrizia Santi ◽  
...  
Keyword(s):  
Mixed Micelles ◽  
Polymeric Micelles ◽  
Ex Vivo ◽  
Preliminary Investigation ◽  
Posterior Segment ◽  
Age Related Macular Degeneration ◽  
Poloxamer 407 ◽  
Low Viscosity ◽  
Age Related ◽  
Ophthalmic Administration

There is increasing consensus in considering statins beneficial for age-related macular degeneration and in general, for immune and inflammatory mediated diseases affecting the posterior segment of the eye. However, all available data relate to oral administration, and safety and effectiveness of statins directly administered to the eye are not yet known, despite their ophthalmic administration could be beneficial. The aim was the development and the characterization of polymeric micelles based on TPGS or TPGS/poloxamer 407 to increase simvastatin solubility and stability and to enhance the delivery of the drug to the posterior segment of the eye via trans-scleral permeation. Simvastatin was chosen as a model statin and its active hydroxy acid metabolite was investigated as well. Results demonstrated that polymeric micelles increased simvastatin solubility at least 30-fold and particularly TPGS/poloxamer 407 mixed micelles, successfully stabilized simvastatin over time, preventing the hydrolysis when stored for 1 month at 4 °C. Furthermore, both TPGS (1.3 mPas) and mixed micelles (33.2 mPas) showed low viscosity, suitable for periocular administration. TPGS micelles resulted the best performing in delivery simvastatin either across conjunctiva or sclera in ex vivo porcine models. The data pave the way for a future viable ocular administration of statins.

Resveratrol-piperine loaded mixed micelles: formulation, characterization, bioavailability, safety and in vitro anticancer activity

RSC Advances ◽  
2016 ◽  
Vol 6 (114) ◽  
pp. 112795-112805 ◽  
Author(s):  
Prakash Jadhav ◽  
C. Bothiraja ◽  
Atmaram Pawar
Keyword(s):  
Polyethylene Glycol ◽  
Anticancer Activity ◽  
Oral Bioavailability ◽  
Mixed Micelles ◽  
Poloxamer 407 ◽  
Polyethylene Glycol 1000

Novel RES-carrying piperine loaded mixed micelles (RES-P-MM) composed of Poloxamer 407 and d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) were developed to enhance the solubility, oral bioavailability and anticancer potency of RES.

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