&lt;p&gt;Superiority of TPGS-loaded micelles in the brain delivery of vinpocetine via administration of thermosensitive intranasal gel&lt;/p&gt;

Ahmed, Tarek A.; El-Say, Khalid M.; Ahmed, Osama A. A.; Aljaeid, Bader M

doi:10.2147/ijn.s213086

Cited by 31 publications

(20 citation statements)

References 56 publications

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“…Structural results show that all systems self-aggregate in small micelles with a core shell structure; the presence of TPGS molecules helps the poloxamer with the formation of monodisperse spherical micelles. The size of the systems is in good agreement with that found in the literature for poloxamer 407 [49], TPGS [50,51] or mixed micelles [7], using microscopic techniques such as TEM or cryo-TEM.…”

Section: Resultssupporting

confidence: 86%

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

et al. 2019

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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.

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Section: Resultssupporting

confidence: 86%

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

et al. 2019

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“…TPGS micelles size has been previously determined both by DLS and by X-ray scattering [ 47 ] and resulted approximately 12 nm. Images from literature [ 21 , 61 ] showed a spherical shape. The results obtained here (T20, T40, T100) are in reasonable agreement with this value ( Table 3 ).…”

Section: Resultsmentioning

confidence: 99%

“…Furthermore, considering the amphiphilic structure of the polymers, an augment of drug retention in the skin could be favored by their capacity to alter the spatial structure of lipids and keratin in the SC reducing its resistance to drug penetration [ 18 , 19 ], in addition to a modification of barrier lipophilicity [ 20 ]. Among the polymers used for micelles preparation, tocopheryl polyethylene glycol 1000 succinate (TPGS), a water-soluble derivative of vitamin E with high biocompatibility and biodegradability, has been widely appreciated in several fields of drug delivery [ 21 , 22 , 23 ] because of solubilization capacity and permeation enhancing property [ 24 ].…”

Section: Introductionmentioning

confidence: 99%

Improvement of Imiquimod Solubilization and Skin Retention via TPGS Micelles: Exploiting the Co-Solubilizing Effect of Oleic Acid

et al. 2021

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Imiquimod (IMQ) is an immunostimulant drug approved for the topical treatment of actinic keratosis, external genital-perianal warts as well as superficial basal cell carcinoma that is used off-label for the treatment of different forms of skin cancers, including some malignant melanocytic proliferations such as lentigo maligna, atypical nevi and other in situ melanoma-related diseases. Imiquimod skin delivery has proven to be a real challenge due to its very low water-solubility and reduced skin penetration capacity. The aim of the work was to improve the drug solubility and skin retention using micelles of d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS), a water-soluble derivative of vitamin E, co-encapsulating various lipophilic compounds with the potential ability to improve imiquimod affinity for the micellar core, and thus its loading into the nanocarrier. The formulations were characterized in terms of particle size, zeta potential and stability over time and micelles performance on the skin was evaluated through the quantification of imiquimod retention in the skin layers and the visualization of a micelle-loaded fluorescent dye by two-photon microscopy. The results showed that imiquimod solubility strictly depends on the nature and concentration of the co-encapsulated compounds. The micellar formulation based on TPGS and oleic acid was identified as the most interesting in terms of both drug solubility (which was increased from few µg/mL to 1154.01 ± 112.78 µg/mL) and micellar stability (which was evaluated up to 6 months from micelles preparation). The delivery efficiency after the application of this formulation alone or incorporated in hydrogels showed to be 42- and 25-folds higher than the one of the commercial creams.

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“…All samples were processed as described in section 2.8.4. The permeated amount of RTG per unit area at various time points was calculated [30,31]. The mean values obtained from analyzed samples were used for statistical analysis.…”

Section: Methodsmentioning

confidence: 99%

DoE‐based validation of a HPLC–UV method for quantification of rotigotine nanocrystals: Application to in vitro dissolution and ex vivo nasal permeation studies

Saha

Pandey

2021

Electrophoresis

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The current work is focused on optimization, development, and validation of a sensitive and specific reversed‐phase high‐performance liquid chromatography (RP‐HPLC) method for the estimation of rotigotine (RTG) in bulk and nanoformulations. The RP‐HPLC method was effectively optimized using the concepts of design of experiments. Critical method variables (CMVs) were screened using Plackett–Burman design. Box–Behnken, a surface response methodology‐based design, was further used for the optimization of CMVs with the number of theoretical plates and retention time (min) as responses. The optimized chromatographic conditions for the RP‐HPLC method were: acetonitrile proportion: 54% v/v, pH of buffer: 5.0 (10 mM), and flow rate: 0.65 mL/min. The number of theoretical plates and retention time in the study were found to be 11206 and 7.65 min, respectively. The developed method exhibited good linearity (R2 = 0.9995) within a range of 25–600 ng/mL and LOD and LOQ were found to be 9 and 12 ng/mL, respectively. The developed RP‐HPLC method was found sensitive, accurate, precise, specific, robust, and stability indicating according to the regulatory guidelines. The validated method was efficiently applied for in vitro dissolution study, ex vivo nasal permeation study, and estimation of drug content of RTG nanocrystals.

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<p>Superiority of TPGS-loaded micelles in the brain delivery of vinpocetine via administration of thermosensitive intranasal gel</p>

Cited by 31 publications

References 56 publications

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

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

Improvement of Imiquimod Solubilization and Skin Retention via TPGS Micelles: Exploiting the Co-Solubilizing Effect of Oleic Acid

DoE‐based validation of a HPLC–UV method for quantification of rotigotine nanocrystals: Application to in vitro dissolution and ex vivo nasal permeation studies

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