The Experts below are selected from a list of 1011 Experts worldwide ranked by ideXlab platform
A. J. Hopfinger - One of the best experts on this subject based on the ideXlab platform.
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A study of the relationship between Cornea Permeability and eye irritation using membrane-interaction QSAR analysis.
Toxicological Sciences, 2005Co-Authors: A. J. HopfingerAbstract:A methodology termed membrane-interaction QSAR (MIQSAR) analysis has been used to develop QSAR models to predict drug Permeability coefficients across Cornea and its component layers (epithelium, stroma, and endothelium). From a training set of 25 structurally diverse drugs, significant QSAR models are constructed and compared for the Permeability of the Cornea, epithelium, and stroma plus endothelium. Cornea Permeability is found to depend on the measured distribution coefficient of the drug, the cohesive energy of the drug, the total potential energy of the drug-membrane ‘‘complex,’’ and three other energy refinement descriptor terms. The endothelium may be a more important barrier in Cornea permeation than the stroma. Moreover, an investigation of the correlation between Cornea permeation and eye irritation is presented as an example of a cross study on different ADMET properties using MI-QSAR analysis. Thirteen structurally diverse drugs, whose molar-adjusted eye irritation scores (MES) have been measured using the Draize rabbit-eye test, were chosen as an eye irritation comparison set. A poor correlation (R 2 ¼ 0.0232) between the MES measures and the predicted Cornea Permeability coefficients for the drugs in the eye irritation
Aida Niroomand - One of the best experts on this subject based on the ideXlab platform.
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loratadine loaded thermoresponsive hydrogel characterization and ex vivo rabbit Cornea Permeability studies
Iranian Journal of Pharmaceutical Research, 2018Co-Authors: Behzad Sharif Makhmalzadeh, Anayatollah Salimi, Aida NiroomandAbstract:Poor bioavailability of ophthalmic drops is mainly due to drainage through the nasal-lacrimal duct and a very low Permeability through Corneal epithelium. The aim of our study was to prepare and characterize an ocular hydrogel of loratadine, as an example of a lipophilic drug, to increase drug concentration and residence time at the site of action in the eye. In this study, a 23 full factorial design was employed to design and compare the properties of eight different loratadine containing hydrogel formulations. Results showed a significant correlation between the swelling and porosity ratios of the hydrogels and the Pluronic percentage and Pluronic/carbomer ratio in the formulations. Moreover, the release profiles showed fast and sustained release of all the formulations. Evaluation of hydrogels structure by the FT-IR technique indicated that Pluronic interacts with hydroxyl and carboxylic groups in carbomer, which is the main reason of the hydrogel network formation and interacts with loratadine.The permeation of loratadine through rabbit Cornea showed that drug permeation percentages for the F2 and F7 formulations were 15 and 70 folds more than that of the control.
Behzad Sharif Makhmalzadeh - One of the best experts on this subject based on the ideXlab platform.
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loratadine loaded thermoresponsive hydrogel characterization and ex vivo rabbit Cornea Permeability studies
Iranian Journal of Pharmaceutical Research, 2018Co-Authors: Behzad Sharif Makhmalzadeh, Anayatollah Salimi, Aida NiroomandAbstract:Poor bioavailability of ophthalmic drops is mainly due to drainage through the nasal-lacrimal duct and a very low Permeability through Corneal epithelium. The aim of our study was to prepare and characterize an ocular hydrogel of loratadine, as an example of a lipophilic drug, to increase drug concentration and residence time at the site of action in the eye. In this study, a 23 full factorial design was employed to design and compare the properties of eight different loratadine containing hydrogel formulations. Results showed a significant correlation between the swelling and porosity ratios of the hydrogels and the Pluronic percentage and Pluronic/carbomer ratio in the formulations. Moreover, the release profiles showed fast and sustained release of all the formulations. Evaluation of hydrogels structure by the FT-IR technique indicated that Pluronic interacts with hydroxyl and carboxylic groups in carbomer, which is the main reason of the hydrogel network formation and interacts with loratadine.The permeation of loratadine through rabbit Cornea showed that drug permeation percentages for the F2 and F7 formulations were 15 and 70 folds more than that of the control.
Guangxi Zhai - One of the best experts on this subject based on the ideXlab platform.
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novel in situ gel systems based on p123 tpgs mixed micelles and gellan gum for ophthalmic delivery of curcumin
Colloids and Surfaces B: Biointerfaces, 2015Co-Authors: Yuwei Duan, Xiaoqing Cai, Guangxi ZhaiAbstract:Curcumin, a natural polyphenol compound, has been widely reported for diverse pharmacological effects and already been investigated for eye diseases. However, the water-insolubility of curcumin and the inherent penetration barriers in Cornea make it difficult for curcumin to enter eye. This work aimed to develop ion-sensitive curcumin-loaded Pluronic P123 (P123)/D-a-tocopheryl polyethylene glycolsuccinate (TPGS) mixed micelle in situ gels (CUR-MM-ISGs) to prolong ocular retention time and improve Cornea Permeability. Central composite design-response surface methodology was applied for the optimization of curcumin-loaded P123/TPGS mixed micelles (CUR-MMs). Characterization tests showed that CUR-MMs were in spherical shape with small size and low critical micelle concentration. After dispersing the micelles in gellan gum solution (0.2%, w/w) at the ratio of 3:1 and 1:1 (v/v), respectively, CUR-MM-ISGs were formed and presented transparent appearance. Sustained release profile was obtained in vitro for both CUR-MM-ISGs (3:1 or 1:1, v/v). The irritation test proved that CUR-MM-ISGs as ophthalmic formulations were gentle and biocompatible towards ocular tissues. In addition, the ex vivo Corneal penetration study indicated that the cumulative drug permeation amount of CUR-MM-ISGs (3:1, v/v) was respectively 1.16-fold and 1.32-fold higher than CUR-MM-ISGs (1:1, v/v) and curcumin solution. It can be concluded from these results that the developed ion-sensitive mixed micelle in situ gel system is a potential ophthalmic delivery carrier for curcumin as a poorly soluble drug.
Anayatollah Salimi - One of the best experts on this subject based on the ideXlab platform.
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loratadine loaded thermoresponsive hydrogel characterization and ex vivo rabbit Cornea Permeability studies
Iranian Journal of Pharmaceutical Research, 2018Co-Authors: Behzad Sharif Makhmalzadeh, Anayatollah Salimi, Aida NiroomandAbstract:Poor bioavailability of ophthalmic drops is mainly due to drainage through the nasal-lacrimal duct and a very low Permeability through Corneal epithelium. The aim of our study was to prepare and characterize an ocular hydrogel of loratadine, as an example of a lipophilic drug, to increase drug concentration and residence time at the site of action in the eye. In this study, a 23 full factorial design was employed to design and compare the properties of eight different loratadine containing hydrogel formulations. Results showed a significant correlation between the swelling and porosity ratios of the hydrogels and the Pluronic percentage and Pluronic/carbomer ratio in the formulations. Moreover, the release profiles showed fast and sustained release of all the formulations. Evaluation of hydrogels structure by the FT-IR technique indicated that Pluronic interacts with hydroxyl and carboxylic groups in carbomer, which is the main reason of the hydrogel network formation and interacts with loratadine.The permeation of loratadine through rabbit Cornea showed that drug permeation percentages for the F2 and F7 formulations were 15 and 70 folds more than that of the control.