FORMULATION AND EVALUATION OF INJECTABLE IN SITU GELLING MATRIX SYSTEM OF DILTIAZEM HYDROCHLORIDE FOR CONTROLLED DRUG RELEASE

2017 ◽  
pp. 981-995
Author(s):  
Sanjana N. K.
Keyword(s):  
Drug Release ◽  
Controlled Drug Release ◽  
Matrix System ◽  
Diltiazem Hydrochloride ◽  
In Situ Gelling

scholarly journals FORMULATION AND EVALUATION OF FLOATING ORAL IN SITU GEL OF DILTIAZEM HYDROCHLORIDE

2016 ◽  
Vol 9 (1) ◽  
pp. 50
Author(s):  
A. Maheswaran ◽  
J. Padmavathy ◽  
V. Nandhini ◽  
D. Saravanan ◽  
P. Angel
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Polymer Concentration ◽  
Methyl Cellulose ◽  
Diltiazem Hydrochloride ◽  
Release Formulation ◽  
Gelling Properties ◽  
In Situ Gelling

Objective: The objective of the present study was to formulate and evaluate the floating in-situ gelling system of diltiazem hydrochloride.Methods: Sodium alginate based diltiazem hydrochloride floating in situ gelling systems were prepared by dissolving hydroxyl propyl methyl cellulose (HPMC) in 25% of water, to which calcium carbonate and diltiazem hydrochloride were added with stirring to form, a proper and a homogenous dispersion of diltiazem hydrochloride. Meanwhile, 30% of water was heated to 60 ˚C on a hot plate to dissolve sodium alginate and cooled to 40 ˚C. The resulting solution was added to HPMC solution and mixed well. To 5% of water at 60 ˚C, sodium methyl paraben was added and dissolved and cooled to 40 ˚C and was added to the above mixture and mixed well. The volume was adjusted finally to 100% with distilled water. Prepared formulae were evaluated for physicochemical properties, drug content, pH, in vitro gelling capacity, in vitro buoyancy, viscosity, water uptake and in vitro drug release.Results: Formulation variables such as type and concentration of viscosity enhancing polymer (sodium alginate) and HPMC affected the formulation viscosity, gelling properties, floating behavior, and in vitro drug release. Formulation F5 and F6 showed the floating time of 5 min and more than 20 h respectively. A significant decrease in the rate and extent of the drug release was observed with the increase in polymer concentration in in-situ gelling preparation. Formulation F4, F5, F6 were shown to have extended drug release until the end of 7 h.Conclusion: The prepared in situ gelling formulations of diltiazem hydrochloride could float in the gastric conditions and released the drug in a sustained manner. The present formulation was non-irritant, easy to administer along with good retention properties, better patient compliant and with greater efficacy of the drug.

scholarly journals Formulation, Ex-Vivo and Preclinical In-Vivo Studies of Combined pH and Ion-Sensitive Ocular Sustained In Situ Hydrogel of Timolol Maleate for the Treatment of Glaucoma

2020 ◽  
Vol 11 (1) ◽  
pp. 8242-8265
Keyword(s):  
Drug Release ◽  
Physiological Condition ◽  
Controlled Drug Release ◽  
Gellan Gum ◽  
Class I ◽  
Timolol Maleate ◽  
In Situ Hydrogel ◽  
In Situ Gelling ◽  
Carbopol 934P

The aim of the present research work was to develop safe, effective, and stable in situ hydrogel for the ophthalmic drug delivery using the combination of ion-responsive polymer gellan gum and pH-sensitive polymer carbopol 934P to treat glaucoma. Background: Timolol maleate is a BCS class I drug used as the first line of treatment in open-angle glaucoma. The rapid precorneal elimination of conventional formulation containing class I drugs exhibits poor therapeutic effect and bioavailability. So, in situ gelling system was formulated and characterized. Methods: Box-Behnken design was used to statistically optimize the formulation parameters and evaluate the effects of formulation attributes, namely concentration of gellan gum (X1), the concentration of carbopol 934P (X2) and concentration of benzododecenium bromide (X3) on selected critical quality attributes (Y1-Y7). Trial run data were statistically analyzed using the polynomial equation and response surface plots. Optimized formulation was selected based on desirability function, design space, and was further characterized and compared with the marketed formulation. Results: The concentration of both polymers showed a synergistic positive impact on viscosity at the non-physiological and physiological conditions. Trial runs showed controlled drug release with diffusion-controlled mechanism and good mucoadhesive strength due to the presence of Carbopol 934P. The preservative benzododecenium bromide showed the ability to enhance trans-corneal permeation. The optimized formulation has appeared as a clear solution at the non-physiological condition and clear gel at the physiological condition with an acceptable pH range of 5-6. Other quality attributes like rheological properties, gelling capacity, texture analysis, Isotonicity, contact angle, sterility, antimicrobial efficacy, and stability were found in desires values for the ocular application. The safety of in situ gel for human use was confirmed by ocular irritation and histopathology studies in the rabbit eyes. The intraocular pressure (IOP) reduction with optimized formulation was found comparable and less fluctuating compared to ophthalmic gel-forming marketed solution of timolol maleate (TIMOPTIC-XE®). Conclusion: The cross-linking between Carbopol 934P with Gellan gum in the formation showed more viscous gelling at the physiological condition to provide long pre-corneal residence time. The optimized formulation exhibited all the desirable attributes of an ideal ophthalmic in situ gelling formulation, exhibited in-vitro controlled drug release, good gelling capacity, and was found to be stable and non-irritant to the eye.

scholarly journals An Injectable and In Situ-Gelling Biopolymer for Sustained Drug Release Following Perineural Administration

Spine ◽  
2008 ◽  
Vol 33 (7) ◽  
pp. 748-754 ◽  
Author(s):  
Mohammed F. Shamji ◽  
Lyman Whitlatch ◽  
Allan H. Friedman ◽  
William J. Richardson ◽  
Ashutosh Chilkoti ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Drug Release ◽  
In Situ Gelling

DESIGN, CHARACTERIZATION AND EVALUATION OF MUCOADHESIVE NASAL IN SITU GELLING FORMULATIONS OF VENLAFAXINE HYDROCHLORIDE FOR BRAIN TARGETTING

INDIAN DRUGS ◽  
2016 ◽  
Vol 53 (01) ◽  
pp. 25-31
Author(s):  
M Priyanka ◽  
◽  
F. S. Dasankoppa ◽  
H. N Sholapur ◽  
NGN Swamy ◽  
...  
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Linear Regression Analysis ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Drug Content ◽  
Venlafaxine Hydrochloride ◽  
In Situ Gelling

The poor bioavailability and the therapeutic effectiveness exhibited by the anti-depressant venlafaxine hydrochloride on oral administration is overcome by the use of ion-activated gel forming systems that are instilled as drops; these undergo gelation in the nasal cavity. The present study describes the design, characterization and evaluation of mucoadhesive nasal in situ gelling drug delivery of venlafaxine hydrochloride using different polymers like sodium alginate, HPMC and pectin in various concentrations. DSC studies revealed compatibility of the drug and excipients used. The in situ gels were characterized for physicochemical parameters, gelling ability, rheological studies, drug content, drug entrapment efficiency, in vitro mucoadhesive strength, water holding capacity, gel expansion coefficient and in vitro drug release studies. The amount of polymer blends was optimized using 23 full factorial design. The influence of experimental factors on percentage cumulative drug release at the end of 2 and 8 hours were investigated to get optimized formulation. The responses were analyzed using ANOVA and polynomial equation was generated for each response using multiple linear regression analysis. Optimized formulation, F9, containing 1.98% w/V sodium alginate, 0.64% w/V hydroxylpropyl methylcellulose, 0.99% w/V pectin showed percentage cumulative drug release of 19.33 and 80.44 at the end of 2 and 8 hours, respectively, which were close to the predicted values. The optimized formulation was subjected to stability study for three months at 300C /75% RH. The stability study revealed no significant change in pH, drug content and viscosity. Thus, venlafaxine hydrochloride nasal mucoadhesive in situ gel could be successfully formulated to improve bioavailability and to target the brain.

scholarly journals Chemiluminescence-initiated and in situ-enhanced photoisomerization for tissue-depth-independent photo-controlled drug release

2019 ◽  
Vol 10 (5) ◽  
pp. 1401-1409 ◽  
Author(s):  
Yufu Tang ◽  
Xiaomei Lu ◽  
Chao Yin ◽  
Hui Zhao ◽  
Wenbo Hu ◽  
...  
Keyword(s):  
Drug Release ◽  
Penetration Depth ◽  
Controlled Drug Release ◽  
Tissue Penetration

Tissue-penetration-depth-independent self-luminescence is highly expected to perform photoisomerization-related bioapplications in vivo to overcome the limitation of shallow tissue-penetration from external photoexcitation.

scholarly journals Formulation and characterization of a novel pH-triggered in-situ gelling ocular system containing Gatifloxacin

1970 ◽  
Vol 1 (3) ◽  
pp. 43-49 ◽  
Author(s):  
Jovita Kanoujia ◽  
Kanchan Sonker ◽  
Manisha Pandey ◽  
Koshy M Kymonil ◽  
Shubhini A Saraf
Keyword(s):  
Drug Release ◽  
Research Work ◽  
Gelling Agent ◽  
In Vitro Drug Release ◽  
Drug Content ◽  
Carbopol 940 ◽  
In Situ Gelling ◽  
Gel Transition

The present research work deals with the formulation and evaluation of in-situ gelling system based on sol-to-gel transition for ophthalmic delivery of an antibacterial agent gatifloxacin, to overcome the problems of poor bioavailability and therapeutic response exhibited by conventional formulations based a sol-to-gel transition in the cul-de-sac upon instillation. Carbopol 940 was used as the gelling agent in combination with HPMC and HPMC K15M which acted as a viscosity enhancing agent. The prepared formulations were evaluated for pH, clarity, drug content, gelling capacity, bioadhesive strength and in-vitro drug release. In-vitro drug release data of optimized formulation (F12) was treated according to Zero, First, Korsmeyer Peppas and Higuchi kinetics to access the mechanism of drug release. The clarity, pH, viscosity and drug content of the developed formulations were found in range 6.0-6.8, 10-570cps, 82-98% respectively. The gel provided sustained drug release over an 8 hour period. The developed formulation can be used as an in-situ gelling vehicle to enhance ocular bioavailability and the reduction in the frequency of instillation thereby resulting in better patient compliance. Key Words: In-situ gelation; Gatifloxacin; Carbopol 940; HPMC K15M. DOI: http://dx.doi.org/10.3329/icpj.v1i3.9661 International Current Pharmaceutical Journal 2012, 1(3): 43-49

scholarly journals DESIGN, DEVELOPMENT, AND EVALUATION OF AN ION-ACTIVATED OPHTHALMIC IN SITU GEL OF MOXIFLOXACIN HYDROCHLORIDE

2019 ◽  
pp. 94-103
Author(s):  
GIRISH KONDALKAR ◽  
ASISH DEV
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Statistical Models ◽  
Bacterial Infections ◽  
Gelling Agent ◽  
Design Development ◽  
Sustained Drug Release ◽  
Exchange Method ◽  
In Situ Gelling

Objective: The objective of this study was to develop an in situ ophthalmic gel of an anti-infective drug, moxifloxacin (MOX) hydrochloride (HCL), for sustained ocular delivery for the treatment of bacterial infections of the eye. Method: In the present work the in situ gelling systems were prepared by ion exchange method with the help of various concentrations of gelling agent gelrite (0.08 g, 0.1 g and 0.12 g) and sodium alginate (0.6 g, 0.8 g and 1 g) as viscosity enhancer were added in the formulation; 9 formulations were prepared according to 32 factorial designs and evaluated. The responses were analyzed for the analysis of variance using Design-Expert version 10 software. Statistical models were generated for each response parameter. Results: Optimized formulation batch F7 (0.12% gelrite and 0.6% sodium alginate) was liquid before addition of simulated tear fluid (STF) and underwent rapid gelation on addition of STF and had given 84.05% cumulative drug release; the formulation was found to be clear, having good in situ gelling capacity, good antibacterial efficacy, having drug content 99.75%; optimized formulation was sterile and showed sustained drug release over 8 h period as compared to marketed eye drop. Conclusions: From the above results, we can concluded that 32 full factorial design and statistical models can be successfully used to optimize the formulations, and it was concluded that the trial batch F7 (0.12% gelrite and 0.6% sodium alginate) is the best formula (percentage cumulative drug release over 84.05%) and it is possible to formulate in situ ophthalmic gels of MOX HCL using gelrite in combination with sodium alginate for the treatment of various bacterial infections of the eyes.

Vehicle-dependent in situ modification of membrane-controlled drug release

1998 ◽  
Vol 51 (1) ◽  
pp. 23-34 ◽  
Author(s):  
G. Imanidis ◽  
S. Helbing-Strausak ◽  
R. Imboden ◽  
H. Leuenberger
Keyword(s):  
Drug Release ◽  
Controlled Drug Release ◽  
In Situ Modification
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