scholarly journals In Situ Liquid Crystal Gel as a New Ophthalmic Drug Delivery System for Pilocarpine Nitrate: Improving Preocular Retention and Ocular Bioavailability

2021 ◽  
Author(s):  
Wenqing Wu ◽  
Wenxuan Cao ◽  
Ye Cai ◽  
Menghe Zhang ◽  
Tiantian Chen ◽  
...  
Keyword(s):  
Liquid Crystal ◽  
Internal Structure ◽  
Residence Time ◽  
Delivery System ◽  
High Efficiency ◽  
Eye Drops ◽  
Eye Irritation ◽  
Irritation Test

Abstract The purpose of this article is to develop an in-situ liquid crystal gel that can be used as a novel ocular delivery system for pilocarpine nitrate (PN). The phytantriol (PT) -based in situ liquid crystal gels were prepared by a vortex method using PT, PEG400, Triglyceride (TAG) and water (in the ratio of 61.15:30:3.85:5, w/w). Firstly, the internal structure of the PN-loaded liquid crystal gel was characterized by polarizing microscope (PLM), small-angle X-ray scattering (SAXS), differential scanning calorimetry (DSC) and rheology. In vitro drug release behavior and ex vivo corneal permeation were investigated. Finally, eye irritation test，preocular residence time evaluation,were studied in vivo and compared with eye drops.Based on various characterization techniques, it is proved that the internal structure of the gel is a hexagonal phase.In vitro release results identified that PN could be released continuously from HII gel over a period of 24 h. The in vitro obvious permeability coefficient of HII gel was 3.19-fold (P < 0.01) higher than that of the eye drops. Compared with eye drops,the HII gel had good bioadhesion and displayed longer residence time on the eyeballs surface using fluorescent labeling technology.In addition, through Corneal hydration level and eye irritation test ., it is conjectured that HII gel will not cause eye irritation. In short, the formulation has the advantages of high efficiency, slow release and non-toxicity, and will become a promising pharmaceutical strategy to improve the efficacy of glaucoma.

scholarly journals In Situ Gelling Ophthalmic Drug Delivery System for the Optimization of Diagnostic and Preoperative Mydriasis: In Vitro Drug Release, Cytotoxicity and Mydriasis Pharmacodynamics

Pharmaceutics ◽  
2020 ◽  
Vol 12 (4) ◽  
pp. 360
Author(s):  
Pierre-Louis Destruel ◽  
Ni Zeng ◽  
Françoise Brignole-Baudouin ◽  
Sophie Douat ◽  
Johanne Seguin ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Delivery System ◽  
Delivery Systems ◽  
Eye Drops ◽  
Active Ingredients ◽  
In Vitro Drug Release ◽  
In Situ Gelling

Mydriasis is required prior to many eye examinations and ophthalmic surgeries. Nowadays, phenylephrine hydrochloride (PHE) and tropicamide (TPC) are extensively used to induce mydriasis. Several pharmaceutic dosage forms of these two active ingredients have been described. However, no optimal therapeutic strategy has reached the market. The present work focuses on the formulation and evaluation of a mucoadhesive ion-activated in situ gelling delivery system based on gellan gum and hydroxyethylcellulose (HEC) for the delivery of phenylephrine and tropicamide. First, in vitro drug release was studied to assess appropriate sustained drug delivery on the ocular surface region. Drug release mechanisms were explored and explained using mathematical modeling. Then, in situ gelling delivery systems were visualized using scanning electron microscopy illustrating the drug release phenomena involved. Afterward, cytotoxicity of the developed formulations was studied and compared with those of commercially available eye drops. Human epithelial corneal cells were used. Finally, mydriasis intensity and kinetic was investigated in vivo. Mydriasis pharmacodynamics was studied by non-invasive optical imaging on vigilant rabbits, allowing eye blinking and nasolacrimal drainage to occur physiologically. In situ gelling delivery systems mydriasis profiles exhibited a significant increase of intensity and duration compared with those of conventional eye drops. Efficient mydriasis was achieved following the administration of a single drop of in situ gel reducing the required amount of administered active ingredients by four- to eight-fold compared with classic eye drop regimen.

scholarly journals Ophthalmic Drug Dosage Forms: Characterisation and Research Methods

2014 ◽  
Vol 2014 ◽  
pp. 1-14 ◽  
Author(s):  
Przemysław Baranowski ◽  
Bożena Karolewicz ◽  
Maciej Gajda ◽  
Janusz Pluta
Keyword(s):  
Defense Mechanisms ◽  
Drug Application ◽  
Drug Dosage ◽  
Eye Drops ◽  
Eye Tissues ◽  
Ophthalmic Drug ◽  
Application Frequency

This paper describes hitherto developed drug forms for topical ocular administration, that is, eye drops, ointments,in situgels, inserts, multicompartment drug delivery systems, and ophthalmic drug forms with bioadhesive properties. Heretofore, many studies have demonstrated that new and more complex ophthalmic drug forms exhibit advantage over traditional ones and are able to increase the bioavailability of the active substance by, among others, reducing the susceptibility of drug forms to defense mechanisms of the human eye, extending contact time of drug with the cornea, increasing the penetration through the complex anatomical structure of the eye, and providing controlled release of drugs into the eye tissues, which allows reducing the drug application frequency. The rest of the paper describes recommendedin vitroandin vivostudies to be performed for various ophthalmic drugs forms in order to assess whether the form is acceptable from the perspective of desired properties and patient’s compliance.

The CTFA evaluation of alternatives program: An evaluation of in vitro alternatives to the draize primary eye irritation test. (Phase II) oil/water emulsions

1994 ◽  
Vol 32 (10) ◽  
pp. 943-976 ◽  
Author(s):  
S.D. Gettings ◽  
L.C. Dipasquale ◽  
D.M. Bagley ◽  
P.L. Casterton ◽  
M. Chudkowski ◽  
...  
Keyword(s):  
Phase Ii ◽  
Test Phase ◽  
Eye Irritation ◽  
Irritation Test ◽  
Oil Water

In Vitro and In Vivo Drug Release from a Novel In Situ Forming Drug Delivery System

2007 ◽  
Vol 25 (6) ◽  
pp. 1347-1354 ◽  
Author(s):  
Heiko Kranz ◽  
Erol Yilmaz ◽  
Gayle A. Brazeau ◽  
Roland Bodmeier
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
In Situ Forming

scholarly journals DEVELOPMENT AND CHARACTERIZATION OF IN SITU GEL OF XANTHAN GUM FOR OPHTHALMIC FORMULATION CONTAINING BRIMONIDINE TARTRATE

2018 ◽  
Vol 11 (7) ◽  
pp. 277 ◽  
Author(s):  
Vazir Ashfaq Ahmed ◽  
Divakar Goli
Keyword(s):  
Drug Release ◽  
Xanthan Gum ◽  
Gelation Time ◽  
Gel Strength ◽  
Eye Drops ◽  
In Situ Gel ◽  
23 Factorial Design ◽  
Brimonidine Tartrate

Objective: The goal of this study was to develop and characterize an ion-activated in situ gel-forming brimonidine tartrate, solution eye drops containing xanthan gum as a mucoadhesive polymer.Method: Sol-gel formulation was prepared using gellan gum as an ion-activated gel-forming polymer, xanthan gum as mucoadhesive agent, and hydroxypropyl methyl cellulose (HPMC E50LV) as release retardant polymer. Phenylethyl alcohol is used as preservatives in borate buffer. The 23 factorial design was employed to optimize the formulation considering the concentration of gelrite, xanthan gum and HPMC as independent variables, gelation time, gel strength, and mucoadhesive force (N). Gelation time , gel strength, mucoadhesive force (N), viscosity (cP) and in vitro percentage drug release were chosen as dependent variables. The formulation was characteristics for pH, clarity, isotonicity, sterility, rheological behavior, and in vitro drug release, ocular irritation, and ocular visualization.Result: Based on desirability index of responses, the formulation containing a concentration of gelrite (0.4%), xanthan gum (0.21%), and HPMC (HPMC E50 (0.24%) was found to be the optimized formulation concentration developed by 23 factorial design. The solution eye drops resulted in an in situ phase change to gel-state when mixed with simulated tear fluid. The gel formation was also confirmed by viscoelastic measurements. Drug release from the gel followed non-fickian mechanism with 88% of drug released in 10 h, thus increased the residence time of the drug.Conclusion: An in situ gelling system is a valuable alternative to the conventional system with added benefits of sustained drug release which may ultimately result in improved patient compliance.

Me-too validation study for in vitro eye irritation test with 3D-reconstructed human cornea epithelium, MCTT HCETM

2019 ◽  
Vol 55 ◽  
pp. 173-184 ◽  
Author(s):  
Song-E Lim ◽  
Su Jin Ha ◽  
Won-Hee Jang ◽  
Kyung-Mi Jung ◽  
Mi-Sook Jung ◽  
...  
Keyword(s):  
Validation Study ◽  
Human Cornea ◽  
Eye Irritation ◽  
Irritation Test ◽  
Cornea Epithelium

Novel Materials for Myco-Decontamination of Cyanide-Containing Wastewaters through Microbial Biotechnology

2021 ◽  
Vol 1037 ◽  
pp. 751-758
Author(s):  
Igor N. Pavlov ◽  
Yulia A. Litovka
Keyword(s):  
Large Scale ◽  
High Efficiency ◽  
Pine Sawdust ◽  
Microbial Biotechnology ◽  
Tailing Dam ◽  
Large Scale Cultivation ◽  
Siberian Pine ◽  
Uniform Ratio

This study examined the effectiveness of decontamination of industrial cyanide-containing water using mycelium-based lignocellulosic materials. These results suggest that fungi biomass and plant substrates can be used successfully in the treatment of wastewater contaminated by cyanide. Fungi were isolated from old wood samples taken from a tailing dam with high cyanide content (more than 20 years in semi-submerged condition). All isolated fungi belonged to the genus Fusarium. Fusarium oxysporum Schltdl. is most effective for biodegradation of cyanide-containing wastewaters (even at low temperatures). The most optimal lignocellulosic composition for production of mycelium-based biomaterial for biodegradation of cyanide wastewater consists of a uniform ratio of Siberian pine sawdust and wheat straw. The high efficiency of mycelium-based materials has been experimentally proven in vitro at 15-25 ° C. New fungal biomaterials are provide decrease in the concentration of cyanide ions to 79% (P <0.001). Large-scale cultivation of fungi biomass was carried out by the periodic liquid-phase cultivation. The submerged biomass from bioreactor was used as an inoculum for the production of mycelium-based materials for bioremediation of cyanide wastewater in situ (gold mine tailing).

scholarly journals GREEN TEA EXTRACT IN AN EYELASH GROWTH ENHANCER GEL FORMULATION: STABILITY TEST, EYE IRRITATION TEST, AND HUMAN EYELASH GROWTH ACTIVITY

2017 ◽  
Vol 10 (6) ◽  
pp. 243
Author(s):  
Indra Syahputra Roes Lie ◽  
Joshita Djajadisastra ◽  
Fadlina Chany Saputri
Keyword(s):  
Green Tea ◽  
Chorioallantoic Membrane ◽  
Test Group ◽  
Green Tea Extract ◽  
Stability Test ◽  
Eye Irritation ◽  
Before And After ◽  
Irritation Test ◽  
Tea Extract

Objective: To formulate a green tea extract (GTE), which is often used as a hair growth product, to produce an eyelash gel with good stability, effectiveness, and safety for growing eyelashes.Methods: GTE was formulated into a gel. A stability test was performed at a high temperature (40±2°C), room temperature (25±2°C), low temperature (4±2°C), and a cycling temperature. An in vitro hen’s egg test-chorioallantoic membrane assay was performed to evaluate potential eye irritation. An eyelash growth test was conducted by length measurement using an eyelash ruler before and after 2 mo of application in human volunteers. Results: The GTE gel was stable in storage at high, room, and low temperatures and at cycling temperatures and did not cause eye irritation. Eyelashes grew significantly more in the test group than in the placebo group after 2 mo of application (p<0.05). Conclusion: GTE gel provides a new, safe, and effective option for growing natural eyelashes.

scholarly journals Preparation of a Sustained Release Drug Delivery System for Dexamethasone by a Thermosensitive, In Situ Forming Hydrogel for Use in Differentiation of Dental Pulp

2013 ◽  
Vol 2013 ◽  
pp. 1-6 ◽  
Author(s):  
Elham Khodaverdi ◽  
Fatemeh Kheirandish ◽  
Farnaz Sadat Mirzazadeh Tekie ◽  
Bibi Zahra Khashyarmanesh ◽  
Farzin Hadizadeh ◽  
...  
Keyword(s):  
Phase Transition ◽  
Transition Temperature ◽  
Phase Transition Temperature ◽  
Delivery System ◽  
In Vitro Release ◽  
In Situ Forming ◽  
Release Study ◽  
Vitro Release

In situ forming delivery systems composed of block copolymers are attracting substantial attention due to their ease of use, biocompatibility, and biodegradability. In this study, the thermoresponsive triblock copolymer PLGA-PEG-PLGA was studied as a dexamethasone delivery system. Dexamethasone, a synthetic glucocorticoid, is used clinically to improve inflammation, pain, and the hyperemesis of chemotherapy, and it is applied experimentally as a differentiation factor in tissue engineering. PLGA-PEG-PLGA was synthesised under microwave irradiation for 5 min. The obtained copolymer was characterised to determine its structure and phase transition temperature. An in vitro release study was conducted for various copolymer structures and drug concentrations. The yield of the reaction and HNMR analysis confirmed the appropriateness of the microwave-assisted method for PLGA-PEG-PLGA synthesis. Phase transition temperature was affected by the drug molecule as well as by the copolymer concentration and structure. An in vitro release study demonstrated that release occurs mainly by diffusion and does not depend on the copolymer structure or dexamethasone concentration.

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