scholarly journals FORMULATION, DEVELOPMENT AND IN-VITRO EVALUATION OF A BAMBUTEROL HYDROCHLORIDE IN-SITU GELLING SYSTEM FOR NASAL DELIVERY

2021 ◽  
Vol 11 (6) ◽  
pp. 5-8
Author(s):  
Vipulata P. Galankar
Keyword(s):  
Gel Strength ◽  
Nasal Delivery ◽  
Nasal Administration ◽  
Formulation Development ◽  
Rotational Viscometer ◽  
In Vitro Evaluation ◽  
In Situ Nasal Gel ◽  
In Situ Gelling

The goal of this project was to design, develop, and in-vitro evaluation of an in-situ gelling system for nasal administration of Bambuterol hydrochloride. All of the batches were prepared using different concentration of pectin, given different doses of simulated nasal electrolyte solution (SNES) i.e., 0.1 ml to 2.0 ml. All batches and formulation batches with a composition of 0.8 percent low methoxyl pectin underwent an in vitro gelation testing. The pH of the formulation reduced as the pectin content increased due to the acidic nature of pectin. The drug concentration was greater than 95%, and the apparent viscosity of the sol and gel was measured using a Brookfield viscometer (Rotational Viscometer Model). When the concentration of gelling polymer was increased from 0.5 to 1.0 percent, the gel strength (SOL) increased from 0.6 to 1 sec. The gel strength (GEL) increased from 0.7 to 13 seconds as a result of gelation. In vitro drug release experiments showed that the resulting formulations could release the medication for up to 10 hours when Higuchi kinetics were applied to all of them. The gels were stable across the six-month test period, according to the accelerated stability studies. There was no drug-polymer interaction, according to DSC and XRD analyses. Based on these findings, in situ nasal gel could be a possible drug delivery strategy for bambuterol hydrochloride, allowing it to bypass first-pass metabolism and hence improve bioavailability.

FORMULATION AND IN-VITRO EVALUATION OF ZOLMITRIPTAN IN SITU GEL FOR NASAL ADMINISTRATION

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (12) ◽  
pp. 54-58
Author(s):  
P. H Patil ◽  
◽  
V. S Belgamwar ◽  
D. A Patel ◽  
S. J. Surana
Keyword(s):  
Evaluation Studies ◽  
Methyl Cellulose ◽  
Nasal Delivery ◽  
Nasal Administration ◽  
Histopathological Study ◽  
In Situ Gel ◽  
In Vitro Evaluation ◽  
Effective Delivery

The aim of present investigation was formulation and in-vitro evaluation of in situ gel for the nasal delivery of zolmitriptan. The in situ gel was prepared by temperature induced gelation technique using Pluronic with mucoadhesive polymer hydroxy propyl methyl cellulose K4 M in different ratios. The in situ gels so prepared were characterized and from the evaluation studies, batch PH2 was optimized and further subjected for stability studies at 30±2°C and 60±5% RH for 90 days. These formulations retained good stability at accelerated conditions and also did not show any remarkable damage to nasal mucosa in histopathological study. Owing to these properties it can be used as an effective delivery system for the nasal route.

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.

In-Situ Gelling System based on Thiolated Gellan Gum as New Carrier for Nasal Administration of Dimenhydrinate

2009 ◽  
Vol 2 (2) ◽  
pp. 544-550
Author(s):  
Hitendra Mahajan ◽  
Hannan Shaikh ◽  
Surendra Gattani ◽  
Pankaj Nerkar
Keyword(s):  
Nasal Mucosa ◽  
Histopathological Examination ◽  
Polymer Concentration ◽  
Gellan Gum ◽  
Nasal Administration ◽  
In Vitro Permeation ◽  
Permeation Studies ◽  
In Situ Gelling

The purpose of the present study was to develop intranasal delivery system of dimenhydrinate using thiolated gellan gum and formulations were modulated so as to have gelation at physiological ion content after intranasal administration.  Gelation was determined by physical appearance.  The mucoadhesive force in terms of detachment stress, determined using sheep nasal mucosa, increased with increasing concentration of thiolated polymer. The results of in vitro drug permeation studies across sheep nasal mucosa indicate that effective permeation could be significantly increased by using in situ gelling formulation with thiolated polymer concentration.  Finally, histopathological examination did not detect any changes during in vitro permeation studies.  In conclusion the gel formulation of dimenhydrinate with in situ gelling and mucoadhesive properties with increased permeation rate is promising for prolonging nasal residence time and thereby nasal absorption.

THERMOREVERSIBLE, MUCOADHESIVE IN SITU GELLING FORMULATIONS FOR NASAL DELIVERY OF PROPRANOLOL HYDROCHLORIDE

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (09) ◽  
pp. 41-51
Author(s):  
R Bhat ◽  
◽  
Z. Abbas ◽  
N.G.N. Swamy
Keyword(s):  
Nasal Delivery ◽  
Propranolol Hydrochloride ◽  
Gelation Temperature ◽  
Enhanced Absorption ◽  
Diffusion Controlled ◽  
Thixotropic Behaviour ◽  
In Situ Gelling ◽  
Carbopol 934P

Mucoadhesive, thermoreversible propranolol hydrochloride formulations were made to overcome firstpass metabolism, to prolong the drug residence time in the nasal cavity and to improve the therapeutic efficacy. In situ gelling formulations were prepared by cold technique using Pluronic F-127, Pluronic F-68 / Polyvinyl Alcohol complex and Carbopol 934P as the mucoadhesive polymer. Formulations were so modulated as to have gelation temperature below 340C to ensure gelation at the physiological temperature after intranasal administration. Gelation was characterized by physical appearance as well as by rheological evaluation. The gelation temperature decreased with increase in Carbopol concentration, whereas mucoadhesive force increased. The formulations displayed a thixotropic behaviour. The pH of the nasal gels was found to be in the range of 5.3 to 5.6 very much ideal for nasal delivery. The results of in vitro drug diffusion studies across the sheep nasal mucosa indicated that the drug release increased with increase in Carbopol concentration. The release was found to be matrix diffusion controlled and occurred by Fickian mechanism. It could be concluded that, the mucoadhesive, in situ gelling formulations of propranolol hydrochloride proved to be physically stable, convenient, effective nasal delivery systems ensuring prolonged nasal residence and assuring enhanced absorption.

scholarly journals Preparation, characterization, and in vivo pharmacokinetics of thermosensitive in situ nasal gel of donepezil hydrochloride

2020 ◽  
Vol 70 (3) ◽  
pp. 411-422 ◽  
Author(s):  
Fugen Gu ◽  
Huimin Fan ◽  
Zhixin Cong ◽  
Shuang Li ◽  
Yi Wang ◽  
...  
Keyword(s):  
Ph Value ◽  
Relative Bioavailability ◽  
Nasal Delivery ◽  
Poloxamer 407 ◽  
Nasal Administration ◽  
Pharmacokinetic Parameters ◽  
Donepezil Hydrochloride

AbstractDonepezil hydrochloride thermosensitive in situ gel for nasal delivery was prepared by using Poloxamer 407 and Poloxamer 188 as thermoreversible polymers, hydroxypropyl-β-cyclodextrin and ethylparaben as permeation enhancer and preservative, respectively. The gelation temperature and time, pH value of the gel formulation were found to meet the requirements for nasal administration. The in vitro erosion and in vitro release tests exhibited obvious drug sustained release behavior. Meantime, main pharmacokinetic parameters such as tmax, cmax and AUC in plasma as well as in brain were significantly different between the nasal gel formulation and intragastric drug solution in rats (p < 0.01). The relative bioavailability and drug targeting efficiency of the gel formulation were calculated to be 385.6 and 151.2 %, respectively. Thus, the drug gel formulation might be a potential new delivery system for treatment of Alzheimer’s disease due to its higher bioavailability and better distribution to brain when compared to oral route.

scholarly journals Formulation and In Vitro Evaluation of Salbutamol Sulphate In Situ Gelling Nasal Inserts

2013 ◽  
Vol 14 (2) ◽  
pp. 712-718 ◽  
Author(s):  
Ragwa M. Farid ◽  
Mohamed A. Etman ◽  
Aly H. Nada ◽  
Abd El Azeem R. Ebian
Keyword(s):  
In Vitro Evaluation ◽  
Salbutamol Sulphate ◽  
In Situ Gelling

Novel Formulation Development and Evaluation of Nanoparticles Based in Situ Gelling System for The Ophthalmic Delivery of Ciprofloxacin Hydrochloride

2015 ◽  
Vol 5 (4) ◽  
Author(s):  
Kranti Singh ◽  
Surajpal Verma ◽  
Shyam Prasad ◽  
Indu Bala
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Drug Loading ◽  
In Vitro Release ◽  
Formulation Development ◽  
Ciprofloxacin Hydrochloride ◽  
Potential Value ◽  
The Mean ◽  
In Situ Gelling

Ciprofloxacin hydrochloride loaded Eudragit RS100 nanoparticles were prepared by using w/o/w emulsification (multiple emulsification) solvent evaporation followed by drying of nanoparticles at 50°C. The nanoparticles were further incorporated into the pH-triggered in situ gel forming system which was prepared using Carbopol 940 in combination with HPMC as viscosifying agent. The developed nanoparticles was evaluated for particle size, zeta potential value and loading efficiency; nanoparticle incorporated in situ gelling system was evaluated for pH, clarity, gelling strength, rheological studies, in-vitro release studies and ex-vivo precorneal permeation studies. The nanopaticle showed the mean particle size varying between 263.5nm - 325.9 nm with the mean zeta potential value of -5.91 mV to -8.13 mV and drug loading capacity varied individually between 72.50% to 98.70% w/w. The formulation was clear with no suspended particles, showed good gelling properties. The gelling was quick and remained for longer time period. The developed formulation was therapeutically efficacious, stable and non-irritant. It provided the sustained release of drug over a period of 8-10 hours.

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