In vitro release of timolol maleate from an in situ gelling polymer system

1993 ◽  
Vol 95 (1-3) ◽  
pp. 219-228 ◽  
Author(s):  
Katarina Lindell ◽  
Sven Engström
Keyword(s):  
In Vitro Release ◽  
Polymer System ◽  
Timolol Maleate ◽  
In Situ Gelling ◽  
Vitro Release

DEVELOPMENT AND INVESTIGATION OF TIMOLOL MALEATE AND TRAVOPROST COMBINATION NIOSOMAL IN SITU GELLING SYSTEM FOR THE TREATMENT OF GLAUCOMA

INDIAN DRUGS ◽  
2015 ◽  
Vol 52 (07) ◽  
pp. 33-35
Author(s):  
A Dubey ◽  
◽  
P Prabhu ◽  
N Nair ◽  
K Beladiya ◽  
...  
Keyword(s):  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Timolol Maleate ◽  
In Situ Gel ◽  
Vesicle Size ◽  
Gelling Time ◽  
In Situ Gelling ◽  
Vitro Release

The aim of the present investigation was to develop a combination of timolol maleate and travoprost niosomal in situ gelling system for the treatment of glaucoma. Niosomes were prepared by thin film hydration technique using rotary flash evaporator. A 32 factorial design was utilized to study the effect of the molar ratio of Span 60 (X1) and cholesterol (X2) on vesicle size, drug entrapment efficiency and in vitro release study. On the basis of vesicle size, maximum entrapment efficiency and in vitro release of drug, best formulations were selected for the preparation of niosomal in situ gel (Drop). On the basis of gelling time and viscosity, optimized ratio of the polymers was selected for the desired preparation. Selected niosomal batches were dispersed in carbopol 940 and HPMC K4M polymer solution (combination IF6) to form in situ gel niosomal formulations (Drop). The gelling time of the niosomal in situ gel (NIF1) was found to be the best (+++) and the viscosity was found to be 1190 cP. Zeta potential, average size analysis, polydispersibility index value was found to be -45.1 mV, 256.5 nm, 0.228 respectively. In vitro drug release was found to be within the range of 50.23 ± 0.54 to 60.23 ± 0.33% over the period of 6 h. IOP lowering activity of best formulation (NIF1) showed more significant and sustained effect than the marketed eye drops. Best formulation (NIF1) was found to be stable, sterile, non irritant and isotonic. Hence niosomal in situ gelling combination system may have the potential of bringing better application than the conventional ocular therapy with improved ocular bioavailability and increased patient compliance.

FORMULATION DEVELOPMENT AND EVALUATION OF AN IN SITU OPHTHALMIC GELLING SYSTEM OF BRIMONIDINE TARTRATE AND TIMOLOL MALEATE FOR THE TREATMENT OF GLAUCOMA

INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (02) ◽  
pp. 76-78
Author(s):  
A Shirodker ◽  
◽  
S. Bhangle ◽  
R. Gude
Keyword(s):  
Hydroxypropyl Methylcellulose ◽  
In Vitro Release ◽  
Content Uniformity ◽  
Formulation Development ◽  
Timolol Maleate ◽  
Release Studies ◽  
Brimonidine Tartrate ◽  
In Situ Gelling

The present study involved formulation of an in situ gelling system of brimonidine tartrate and timolol maleate for the treatment of glaucoma. Carbopol® 980 NF, xanthum gum and hydroxypropyl methylcellulose K4 M were used as polymers. The prepared in situ gelling systems were evaluated for clarity, appearance, texture analysis, pH, viscosity, rheological properties, in vitro gelation, isotonicity, drug content uniformity, in vitro release studies, microbiological evaluation, ex vivo release studies and stability testing. The results of the attenuated total reflectance spectroscopy and differential scanning calorimetry studies confirmed that there is no incompatibility between the drugs and the excipients. The formulations exhibited pseudoplastic rheology and formulation 3 showed the highest release of both the drugs from the formulation. The stability studies showed that the formulation was stable over the given period of time. Thus, it is evident that the in situ gelling system is a promising drug delivery system for the treatment of glaucoma.

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.

scholarly journals Biodegradable Injectable In Situ Implants and Microparticles for Sustained Release of Montelukast: In Vitro Release, Pharmacokinetics, and Stability

2014 ◽  
Vol 15 (3) ◽  
pp. 772-780 ◽  
Author(s):  
Tarek A. Ahmed ◽  
Hany M. Ibrahim ◽  
Ahmed M. Samy ◽  
Alaa Kaseem ◽  
Mohammad T. H. Nutan ◽  
...  
Keyword(s):  
Sustained Release ◽  
In Vitro Release ◽  
Vitro Release

scholarly journals Studies on Mefenamic Acid Microparticles: Formulation, In Vitro Release, and In Situ Studies in Rats

2009 ◽  
Vol 10 (1) ◽  
pp. 104-112 ◽  
Author(s):  
Ferhan Sevgi ◽  
Aysu Yurdasiper ◽  
Buket Kaynarsoy ◽  
Ezgi Turunç ◽  
Tamer Güneri ◽  
...  
Keyword(s):  
Mefenamic Acid ◽  
In Vitro Release ◽  
In Situ Studies ◽  
Vitro Release

scholarly journals OPTIMIZATION AND CHARACTERIZATION OF ION ACTIVATED OCULAR IN-SITU GEL FORMULATION FOR BACTERIAL CONJUNCTIVITIS

2020 ◽  
pp. 182-191
Author(s):  
ANKITA KAPOOR ◽  
G. D. GUPTA
Keyword(s):  
Research Work ◽  
In Vitro Release ◽  
Gellan Gum ◽  
Log P ◽  
Eye Drops ◽  
Bacterial Conjunctivitis ◽  
In Situ Gel ◽  
Vitro Release

Objective: The present research work aims at describing the formulation, optimization and evaluation of ion activated ocular in-situ gel of gatifloxacin for treatment of bacterial conjunctivitis so as to overcome patient inconvenience, precorneal drug elimination, variation in efficacy, vision blurring and frequent instillation associated with conventional eye drops and ointments. Methods: In-situ gel was prepared using gellan gum as an ion activated phase transition polymer and HPMC K100M as release retardant. Gatifloxacin was characterized by spectrophotometry. Crystalline state of the drug was determined using X Ray Diffraction study. The developed formulation exhibited instantaneous gel formation in simulated lacrimal fluid (pH 7.4), which was further evaluated for its rheology, irritancy parameters, in vitro release, trans-corneal permeation and antimicrobial activity. Results: Gatifloxacin exhibited λmax 286 nm obeying Beer Lambert’s law and pH-dependent solubility at a pH range of 2 to 4. 0.6% gellan gum and 0.4% HPMC K100M were optimized in the formulation which exhibited a viscosity of 55 cps in sol form and 325 cps in gel form with pseudoplastic behavior and prolonged in vitro release. Permeation of formulation was 75.8% in 7 h with log P of drug 0.59. Developed isotonic and non-irritant formulation had a lower apparent permeability coefficient of 8.15 x 10-5 cm/sec as compared to marketed formulation. Conclusion: A Formulation can be viewed as an efficacious medicine by virtue of its higher zone of inhibition, ability to enhance precorneal residence time and consequently ocular bioavailability with lesser frequency of administration attributed to slow and prolonged diffusion of the drug from the polymeric solutions.

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