Portrayal and Demonstration of a Novel Procedure for In-Situ Estimation of Gelation Time

Author(s):  
A. AlSofi ◽  
J. Wang ◽  
H. AlHashim ◽  
Z. Kaidar
Keyword(s):  
Author(s):  
Vazir Ashfaq Ahmed ◽  
Divakar Goli

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.


Author(s):  
Hema a Nair ◽  
NAZIA BEGUM

Objective: The present study is intended to investigate the applicability of poloxamer- and chitosan-based temperature induced in situ injectable gelling depot for once a week therapy as an intramuscular injection employing olanzapine as a model drug. Methods: The thermosetting gel was prepared by admixture of a solution of poloxamer P127 and a solution of olanzapine and chitosan in aqueous acetic acid. The resultant formulation was characterized for gelation temperature, gelation time, viscosity, syringeability, pH, drug content, and in vitro drug release. The in vitro release of olanzapine from the gelled depot was followed using USP paddle type II apparatus in conjunction with a dialysis bag. The gel was injected ex vivo into chicken muscle and observed by subsequent dissection. Results: The formulation was designed to have a phase transition temperature of 34°C and gelled in <10 s at 37°C. Addition of chitosan imparted favorable rheological properties to the poloxamer gel and resulted in a pseudoplastic mixture with low viscosity in the sol state and higher viscosity post gelation. The preparation had a pH of 5.4, appropriate drug content and readily passed through a 20 gauge needle. The release of olanzapine was unhindered by the dialysis bag. Following an initial bust, a sustained, zero-order release of the remainder of drug was observed up to 9 days. The injectable was found to form a compact depot when evaluated ex vivo. Conclusion: The developed system showed several features which make it a suitable vehicle for sustained intramuscular delivery of drugs.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (7) ◽  
pp. 969
Author(s):  
Marzia Cirri ◽  
Francesca Maestrelli ◽  
Giulia Nerli ◽  
Natascia Mennini ◽  
Mario D’Ambrosio ◽  
...  

A thermosensitive, mucoadhesive in-situ gel for clonazepam (CLZ) intranasal delivery was developed, which aimed to achieve prolonged in-situ residence and controlled drug release, overcoming problems associated with its oral or parenteral administration. Poloxamer was selected as a thermosensitive polymer and chitosan glutamate and sodium hyaluronate as mucoadhesive and permeation enhancer. Moreover, randomly methylated β-Cyclodextrin (RAMEB) was used to improve the low drug solubility. A screening DoE was applied for a systematic examination of the effect of varying the formulation components proportions on gelation temperature, gelation time and pH. Drug-loaded gels at different clonazepam-RAMEB concentrations were then prepared and characterized for gelation temperature, gelation time, gel strength, mucoadhesive strength, mucoadhesion time, and drug release properties. All formulations showed suitable gelation temperature (29–30.5 °C) and time (50–65 s), but the one with the highest drug-RAMEB concentration showed the best mucoadhesive strength, longest mucoadhesion time (6 h), and greatest release rate. Therefore, it was selected for cytotoxicity and permeation studies through Caco-2 cells, compared with an analogous formulation without RAMEB and a drug solution. Both gels were significantly more effective than the solution. However, RAMEB was essential not only to promote drug release, but also to reduce drug cytotoxicity and further improve its permeability.


2019 ◽  
Vol 9 (7) ◽  
pp. 958-967
Author(s):  
Huali Chen ◽  
Dengwei He ◽  
Ye Zhu ◽  
Weiyang Yu ◽  
Murugan Ramalingam ◽  
...  

Osteochondral defect (OD) refers to damage in the area of articular cartilage extended to the subchondral bone, affecting millions of people worldwide. In situ osteochondral tissue engineering approach, which aims to activate the body's native stem cells and recruit them to the defective site by utilizing biomaterials, has become a potential strategy for repairing focal chondral lesions. However, due to the lack of cell-instructive potential, most of the biomaterials fail to recruit stem cells from the host environment and trigger the cellular and molecular functions necessary for tissue regeneration. In this study, the authors report a new formulation of injectable biomaterial system, based on stromal cell-derived factor-1 (SDF-1)-encapsulated poly(lactic-co-glycolic acid) (PLGA) microspheres loaded chitosan-gelatin (CS-GEL) composite hydrogel system (SDF-1/CS-GEL@PLGA), with the aim of imparting in situ cell-instructive and osteochondral tissue regenerative potential. The osteochondral regenerative potential of SDF-1/CS-GEL@PLGA was studied in rabbit as a model animal and the results were compared with the CS-GEL@PLGA without the SDF-1. The results of this study showed that the CS-GEL@PLGA hydrogel had better gelation time and longer release cycle (>30 days) than the CS-GEL. In addition, SDF-1/CS-GEL@PLGA hydrogels promoted the repair of osteochondral defects in rabbits within 12 weeks as compared to the CS-GEL@PLGA hydrogels. Therefore, based on the experimental data, SDF-1/CS-GEL@PLGA hydrogel is a promising injectable biomaterial system for osteochondral repair and regeneration.


2017 ◽  
Vol 2017 ◽  
pp. 1-7 ◽  
Author(s):  
Baoguo Chen ◽  
Xiaohong Hu

On account of minimally invasive procedure and of filling irregular defects of tissues, injectable hydrogels are increasingly attractive in biomedical fields. However, traditional hydrogel formed by simple physical interaction or in situ crosslinking had inevitably some drawbacks such as low mechanical strength and lack of multifunctional properties. Though many investigations had successfully modified traditional injectable hydrogel to obtain both mechanical and functional properties, an acetalated β-cyclodextrin (Ac-β-CD) nanoparticle composite injectable hydrogel designed in the research was another effective and efficient choice to solve the drawbacks. First of all, gelatin derivative (G-AA) and Ac-β-CD were synthesized to prepare hydrogel and nanoparticle, respectively. In order to ensure good compatibility between nanoparticle and macromonomer and provide crosslink points between nanoparticle and macromonomer, G-AA was simultaneously functionalized onto the surface of Ac-β-CD nanoparticle during the fabrication of Ac-β-CD nanoparticle using one-step method. Finally, injectable composite hydrogel was obtained by photoinitiated polymerization in situ. Hydrogel properties like gelation time and swelling ratio were investigated. The viscoelastic behavior of hydrogels confirmed that typical characteristics of crosslinked elastomer for all hydrogel and nanoparticle in hydrogel could improve the mechanical property of hydrogel. Moreover, the transparency with time had verified obvious acid-response properties of hydrogels.


Author(s):  
Akshay Kumar S ◽  
Vishal Gupta N ◽  
Gowda Dv ◽  
Praveen Sivadasu

Objective: The objective of the present work was to develop an in situ gel composed of Pluronic F-127, Carbopol 934, and methylparaben and loaded with fluconazole using DoE software to sustain the delivery of drug in the buccal cavity.Methods: In situ gels were prepared by temperature-induced method, by employing DoE and characterized by Fourier transform infrared (FTIR), differential scanning calorimeter (DSC), and evaluated for gelation temperature, gelation time, adhesive force, and in vitro diffusion studies.Results: Both FTIR and DSC studies suggested that there were no chemical interactions present between both drug and polymers. The formulated gels S1, S3, and S9 showed gelation at a body temperature. The viscosity, gel strength, and mucoadhesive force for the formulated in situ gels were found to be within the ranges of 375–738 cps, 35–62 s, and 4650–5210.32 dynes/cm2, respectively. The in vitro diffusion studies indicated that optimized in situ gel S3 exhibited the improved ability to sustain the drug compared to other formulations.Conclusion: Thus, developed in situ gel system was determined to be effective in terms of eradication of oral thrush.


2010 ◽  
Vol 64 (5) ◽  
Author(s):  
Huai-Qing Yu ◽  
Rimin Cong

AbstractAn acryloyl end-capped four-arm star-shaped poly(ethylene glycol)-branched-oligo(l-lactide) (4A-PEG-PLA) macromer was firstly prepared. A novel kind of hydrogels was synthesized via the Michael-type addition reaction between (2S,3S)-1,4-bis-sulfanylbutane-2,3-diol (dithiothreitol) and this macromer. Gelation time was determined visually as the time when the precursor solution did not flow on inverting the vials. Hydrogel structure was characterized by FTIR analysis, swelling and degradation tests. It was found that colorless and transparent hydrogels were quickly generated in situ. The gelation time, swelling and degradation behaviors of this kind of hydrogels could be adjusted by changing the concentration of the macromer solution in PBS buffer (pH 7.4). This novel hydrogel is expected to be used as a biomedical material.


Author(s):  
Gorle Ashish ◽  
Yadav Rahul ◽  
Rathod Mukesh ◽  
Mali Prakash

Objective: The present study describes the use of in-situ gel in periodontal drug delivery systems which contains gellan gum (0.4–0.6% w/v), pluronic F127 (14, 15 and 16% w/v), and drug Ciprofloxacin HCl (0.1% w/v). Number of peoples around the world suffered from dental problem and ultimate fear is tooth loss hence in-situ gelling system was designed for the treatment of periodontal diseases. The therapeutic efficacy of drug can be greatly improved by prolonging its contact time.Methods: Formulations were developed by simple solution method. Each formulation was characterized in terms of in gelling strength, viscosity, rheology, content uniformity, in vitro drug release, and syringeability.Results: In vitro gelation time and the nature of the gel formed in simulated saliva for prepared formulations showed polymeric concentration dependency. Drug release data from all formulations was fitted to different kinetic models and the Korsemeyer-Peppas model was the best fit model. Drug release was significantly decreased as the concentration of each polymer component was increased. Increasing the concentration of each polymeric component significantly increased viscosity, syringeability, and time for 50%, 70%, and 90% drug release. In conclusion, the formulations described offer a wide range of physical and drug release characteristics. The formulation containing 0.6% w/v of gellan gum and 14% w/v of pluronic F127 exhibited superior physical characteristics. The formulation stored at 4˚C before application, which is syringeable through 21 gauge needle.Conclusion: This formulation was made to inject directly in to periodontal pocket where it immediately converts in to gel form at body temperature. 


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