scholarly journals FORMULATION AND DEVELOPMENT OF IN SITU FORMING GEL FOR THE TREATMENT OF ORAL THRUSH

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.

2021 ◽  
Vol 12 (3) ◽  
pp. 1861-1869
Author(s):  
Anilkumar J. Shinde ◽  
Karan B. Swami ◽  
Firoj A. Tamboli ◽  
Harinath N. More

The objective of the present study was to development of Zolmitriptan (ZMT) niosomal in situ nasal gel formulation for migraine treatment. By intranasal route delivered drug to the central nervous system (CNS) through the olfactory lobes, which bypasses the first-pass metabolism and consequently enhances the bioavailability. Noisome of ZMT were prepared by using the lipid film hydration method. Optimized niosomal formulation was used to prepare in situ gel. The developed Noisomal formulations were characterized for vesicle size, shape, zeta potential, entrapment efficiency, drug content and in-vitro diffusion study, mucoadhesive strength, permeation study, FTIR, DSC and XRD studies. The FTIR and DSC studies predicted that there was no any interaction in drug and excipients. ZMT niosomes were showed particle size, Polydispersity index (PDI), Zeta potential, % entrapment efficiency and drug content, 149nm, 0.223, -28.9, 88.16±0.8 % and 96.23±1.2% respectively. In-vitro  diffusion study of niosomes shows 96.23±0.7% at 8h. The permeation rate of in situ niosomes gel and the pure drug was about 98.56% and 79.46%, respectively. XRD & DSC studies were showed that reduce crystalinity in the formulations. The SEM images of niosomes were found spherical in shape to some extent showing particle size distribution. Thus, it can be concluded that developed ZMT niosomal in situ gel formulation can be considered as a promising system for which may reduce dose requirement, improve patient acceptability and efficient targeting drug delivery to the brain through the olfactory lobe for migraine treatment.


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.


2013 ◽  
Vol 545 ◽  
pp. 63-68 ◽  
Author(s):  
Jongjan Mahadlek ◽  
Juree Charoenteeraboon ◽  
Thawatchai Phaechamud

Periodontitis is an inflammatory disease of the supporting structures of the tooth caused by bacterial infection which can result in tooth loss. The local intra-pocket drug delivery system was interesting and highly effective for periodontitis treatment. In situ forming gel system is the polymeric solution which could transform into gel for localizing and sustaining the drug release at desired site. This system has been recommended as one of suitable delivery system for this purpose. Benzoyl peroxide (BPO) in situ forming gels were developed using Eudragit RS as polymer dispersed in N-methyl-pyrrolidone (NMP). Peppermint oil and polyethylene glycol 1500 were also incorporated as the excipients. The prepared systems were evaluated for rheology, syringeability (using texture analyzers), in situ gel formation (after injection into PBS pH 6.8), antimicrobial activity (against Streptococcus mutans with agar diffusion) and drug release (with dialysis method in PBS pH 6.8 at 50 rpm, 37 °C). The viscosity and syringeability of the prepared systems was increased as the amount of BPO, peppermint oil or PEG 1500 was increased. All prepared gels showed the Newtonian flow which the viscosity was decreased as the temperature was increased. All prepared gels comprising peppermint oil and PEG 1500 could form in situ gel in used medium which the pH was close to the environment pH of periodontal pocket. The inhibition zone against Streptococcus mutans of the prepared system was significantly decreased when the peppermint oil and PEG 1500 was incorporated owing to the higher viscous environment and thereafter retardation of drug diffusion was evident. This effect could prolong the drug release. From drug release test, all prepared gels could sustain the BPO release for at least 96 hrs. Release kinetic obtained from curve fitting with various release equations using least square fit technique indicated that the release patterns were as Higuchi’s model therefore the release of BPO was performed with diffusion control. This developed BPO in situ forming gel presented its ability as the controlled drug delivery system for localized antimicrobial activity at periodontal pocket.


2020 ◽  
Vol 17 (2) ◽  
pp. 174-183
Author(s):  
Elham Khodaverdi ◽  
Khadijeh Delroba ◽  
Fatemeh Mohammadpour ◽  
Bahman Khameneh ◽  
Sayyed A. Sajadi Tabassi ◽  
...  

Objective: An injectable long acting In-Situ Forming Gel (ISFG) of human Growth Hormone (hGH) was prepared by using triblock PCL-­‐PEG-­‐PCL (Mw 1500-1500-1500). Ring-Opening Polymerization (ROP) of triblock using microwave was applied. Methods: The BCA protein assay Kit was used to determine the concentration of hGH in the in-vitro release medium. Finally, Sodium Dodecyl Sulfate-Polyacrylamide Gel Electrophoresis (SDS-PAGE) tests and Circular Dichroism (CD) spectrum were done to approve the stability of released hGH. The result of ROP demonstrated that the proportion of PCL to PEG accorded with the initial molar ratio of the monomers. The cross-section of the Surface Electron Microscopy (SEM) indicated the porous framework of the hydrogel could load the drug into its tridimensional matrixes structure. There is the low initial burst release of hGH from the supramolecular hydrogel. Results: The maximum in-vitro release of hGH was 71.2 % ± 1.5 that were due to hGH degrading after this time (21 days). The CD spectrum and SDS-PAGE results confirmed the stability of hGH during invitro release evaluation. Conclusion: The results suggest that the sustained-release formulation using PCL-PEG-PCL can be applied to control the release of hGH.


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. 


2010 ◽  
Vol 20 (16) ◽  
pp. 3265 ◽  
Author(s):  
Ju Young Lee ◽  
Yun Mi Kang ◽  
E Sle Kim ◽  
Mi Lan Kang ◽  
Bong Lee ◽  
...  

2016 ◽  
Vol 85 ◽  
pp. 271-276 ◽  
Author(s):  
Zhixia Geng ◽  
Xiaoqing Luo ◽  
Zhenrui Zhang ◽  
Huimin Li ◽  
Jing Tian ◽  
...  

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