scholarly journals Development of a Mucoadhesive and an in Situ Gelling Formulation Based on κ-Carrageenan for Application on Oral Mucosa and Esophagus Walls. II. Loading of a Bioactive Hydroalcoholic Extract

Marine Drugs ◽  
2019 ◽  
Vol 17 (3) ◽  
pp. 153 ◽  
Author(s):  
Barbara Vigani ◽  
Silvia Rossi ◽  
Matteo Gentile ◽  
Giuseppina Sandri ◽  
Maria Bonferoni ◽  
...  
Keyword(s):  
Protective Action ◽  
Extraction Yield ◽  
Dermal Fibroblasts ◽  
Ultrasound Assisted Extraction ◽  
Hydroalcoholic Extract ◽  
Assisted Extraction ◽  
Anti Inflammatory ◽  
In Situ Gelling

The aim of the present work was to load a Hibiscus sabdariffa (HS) hydroalcoholic extract into in situ gelling formulations for the treatment of oral mucositis and esophagitis. Such formulations, selected as the most promising options in a previous work of ours, were composed by κ-carrageenan (κ-CG), a sulfated marine polymer able to gelify in presence of saliva ions, hydroxypropyl cellulose (HPC), used as mucoadhesive agent, and CaCl2, salt able to enhance the interaction κ-CG/saliva ions. HS extract, which is rich in phytochemicals such as polyphenols, polysaccharides and organic acids, was selected due to its antioxidant and anti-inflammatory properties. For HS extraction, three different methodologies (maceration, Ultrasound Assisted Extraction (UAE) and Microwave Assisted Extraction (MAE)) were compared in terms of extraction yield and extract antioxidant activity, revealing that MAE was the best procedure. Rheological and mucoadhesive properties of HS-loaded formulations were investigated. Such formulations were characterized by a low viscosity at 25 °C, guaranteeing an easy administration, a proper in situ gelation behavior and marked elastic and mucoadhesive properties at 37 °C, functional to a protective action towards the damaged mucosa. Finally, the biocompatibility and the proliferative effect of HS-loaded formulations, as well as their antioxidant and anti-inflammatory properties, were proved in vitro on human dermal fibroblasts.

scholarly journals Development of a Mucoadhesive and In Situ Gelling Formulation Based on κ-Carrageenan for Application on Oral Mucosa and Esophagus Walls. I. A Functional In Vitro Characterization

Marine Drugs ◽  
2019 ◽  
Vol 17 (2) ◽  
pp. 112 ◽  
Author(s):  
Barbara Vigani ◽  
Angela Faccendini ◽  
Silvia Rossi ◽  
Giuseppina Sandri ◽  
Maria Bonferoni ◽  
...  
Keyword(s):  
Oral Mucositis ◽  
Protective Action ◽  
Rheological Characterization ◽  
Low Viscosity ◽  
In Vitro Characterization ◽  
Biological Substrates ◽  
Clinically Significant ◽  
In Situ Gelling

Oral mucositis and esophagitis represent the most frequent and clinically significant complications of cytoreductive chemotherapy and radiotherapy, which severely compromise the patient quality of life. The local application of polymeric gels could protect the injured tissues, alleviating the most painful symptoms. The present work aims at developing in situ gelling formulations for the treatment of oral mucositis and esophagitis. To reach these targets, κ-carrageenan (κ-CG) was selected as a polymer having wound healing properties and able to gelify in the presence of saliva ions, while hydroxypropyl cellulose (HPC) was used to improve the mucoadhesive properties of the formulations. CaCl2 was identified as a salt able to enhance the interaction between κ-CG and saliva ions. Different salt and polymer concentrations were investigated in order to obtain a formulation having the following features: (i) low viscosity at room temperature to facilitate administration, (ii) marked elastic properties at 37 °C, functional to a protective action towards damaged tissues, and (iii) mucoadhesive properties. Prototypes characterized by different κ-CG, HPC, and CaCl2 concentrations were subjected to a thorough rheological characterization and to in vitro mucoadhesion and washability tests. The overall results pointed out the ability of the developed formulations to produce a gel able to interact with saliva ions and to adhere to the biological substrates.

scholarly journals Optimisation of ultrasound-assisted extraction of protein from Spirulina platensis using RSM

2018 ◽  
Vol 36 (No. 1) ◽  
pp. 98-108 ◽  
Author(s):  
Aysun Yucetepe ◽  
Oznur Saroglu ◽  
Fatih Bildik ◽  
Beraat Ozcelik ◽  
Ceren Daskaya-Dikmen
Keyword(s):  
Spirulina Platensis ◽  
Phenolic Content ◽  
Protein Digestibility ◽  
Extraction Yield ◽  
Total Phenolic ◽  
In Vitro Protein Digestibility ◽  
Ultrasound Assisted Extraction ◽  
Assisted Extraction ◽  
Vitro Protein

The protein extraction from the blue-green microalgae Spirulina platensis was carried out using ultrasound-assisted extraction and response surface methodology (RSM) was used to optimise extraction conditions. Extraction yield, total phenolic content, antioxidant activity and in vitro protein digestibility of protein extracts were determined. A three factors Box-Behnken design (BBD) of experiments was employed at pH values of 7, 8 and 9; temperatures of 25, 35, and 45°C; and for durations of 60, 90 and 120 minutes. Based on the RSM analysis, optimum extraction conditions (temperature 45°C, pH 7.46 and time 120 min) were obtained for extraction yield (29.05%), total phenolic content (3.52 mg caffeic acid equivalent/g dw), antioxidant activity (11.32 mg Trolox equivalent/g dw) and in vitro protein digestibility (99.36%). We report the first evaluation of the in vitro protein digestibility of Spirulina platensis and find it to be over 90%. This value is higher than the in vitro protein digestibility values of proteins obtained from other algae and plant species, and, in particular, is greater than that of commercial soybean protein isolate.

scholarly journals Evaluation and characterisation of candidate prebiotics extracted from coconut husk by ultrasound-assisted extraction technique

2021 ◽  
Vol 1195 (1) ◽  
pp. 012027
Author(s):  
S L Tang ◽  
C C Koh ◽  
S L Hii
Keyword(s):  
Enzymatic Digestion ◽  
Extraction Yield ◽  
Bacterial Strains ◽  
Human Gastrointestinal Tract ◽  
Beneficial Bacteria ◽  
Ultrasound Assisted Extraction ◽  
Coconut Husk ◽  
Assisted Extraction ◽  
Ultrasound Assisted

Abstract Oligosaccharides are carbohydrates containing between three to ten sugar moieties. Certain oligosaccharides such as inulin and fructo-oligosaccharides are known as prebiotics that promote the growth of beneficial bacteria in the human gastrointestinal tract. This study began by comparing the efficiency of two different solvents (distilled water and 10% w/v sodium hydroxide) in extracting oligosaccharides from the coconut husk by ultrasound-assisted extraction (UAE). Following that, the coconut husk extract (CHE) extract was subjected to a series of prebiotic evaluation tests. The findings indicated that a significantly high extraction yield (40.51 ± 6.00%) could be achieved with 10% w/v NaOH treatment. The in vitro enzymatic digestion study found that there was 43.70 ± 0.15% of hydrolysis at pH 8 after five hours of incubation. For the in vitro gastric juice digestion, 29.21 ± 0.71% of hydrolysis was recorded at pH 1 after four hours of incubation. The extract was able to stimulate the growth of selected beneficial bacterial strains. FTIR and NMR analysis of the CHE revealed that the extract has a similar structure to the well-known prebiotic inulin.

Natural Anti-inflammatory compounds as Drug candidates in Alzheimer’s disease

2020 ◽  
Vol 27 ◽  
Author(s):  
Reyaz Hassan Mir ◽  
Abdul Jalil Shah ◽  
Roohi Mohi-ud-din ◽  
Faheem Hyder Potoo ◽  
Mohd. Akbar Dar ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Natural Products ◽  
Protective Action ◽  
New Drugs ◽  
Huperzine A ◽  
Brain Disorder ◽  
Anti Inflammatory

: Alzheimer's disease (AD) is a chronic neurodegenerative brain disorder characterized by memory impairment, dementia, oxidative stress in elderly people. Currently, only a few drugs are available in the market with various adverse effects. So to develop new drugs with protective action against the disease, research is turning to the identification of plant products as a remedy. Natural compounds with anti-inflammatory activity could be good candidates for developing effective therapeutic strategies. Phytochemicals including Curcumin, Resveratrol, Quercetin, Huperzine-A, Rosmarinic acid, genistein, obovatol, and Oxyresvertarol were reported molecules for the treatment of AD. Several alkaloids such as galantamine, oridonin, glaucocalyxin B, tetrandrine, berberine, anatabine have been shown anti-inflammatory effects in AD models in vitro as well as in-vivo. In conclusion, natural products from plants represent interesting candidates for the treatment of AD. This review highlights the potential of specific compounds from natural products along with their synthetic derivatives to counteract AD in the CNS.

scholarly journals Mathematical Modelling of Ultrasound-Assisted Extraction Kinetics of Bioactive Compounds from Artichoke By-Products

Foods ◽  
2021 ◽  
Vol 10 (5) ◽  
pp. 931
Author(s):  
Cristina Reche ◽  
Carmen Rosselló ◽  
Mónica M. Umaña ◽  
Valeria Eim ◽  
Susana Simal
Keyword(s):  
Power Density ◽  
Bioactive Compounds ◽  
Extraction Yield ◽  
Total Phenolic ◽  
Model Parameters ◽  
Ultrasound Assisted Extraction ◽  
Yield Curves ◽  
Assisted Extraction ◽  
Ultrasound Assisted ◽  
Ultrasound Power

Valorization of an artichoke by-product, rich in bioactive compounds, by ultrasound-assisted extraction, is proposed. The extraction yield curves of total phenolic content (TPC) and chlorogenic acid content (CAC) in 20% ethanol (v/v) with agitation (100 rpm) and ultrasound (200 and 335 W/L) were determined at 25, 40, and 60 °C. A mathematical model considering simultaneous diffusion and convection is proposed to simulate the extraction curves and to quantify both temperature and ultrasound power density effects in terms of the model parameters variation. The effective diffusion coefficient exhibited temperature dependence (72% increase for TPC from 25 °C to 60 °C), whereas the external mass transfer coefficient and the equilibrium extraction yield depended on both temperature (72% and 90% increases for TPC from 25 to 60 °C) and ultrasound power density (26 and 51% increases for TPC from 0 (agitation) to 335 W/L). The model allowed the accurate curves simulation, the average mean relative error being 5.3 ± 2.6%. Thus, the need of considering two resistances in series to satisfactorily simulate the extraction yield curves could be related to the diffusion of the bioactive compound from inside the vegetable cells toward the intercellular volume and from there, to the liquid phase.

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 Optimization of ultrasound-assisted extraction of procyanidins from perilla seed hull and their antioxidant activities in vitro

2019 ◽  
Vol 39 (2) ◽  
pp. 378-387 ◽  
Author(s):  
Hui-Zhen LI ◽  
Yong-Lan TAN ◽  
Zhi-Jun ZHANG ◽  
Yao-Yao XIA ◽  
Xiao-Jun LI ◽  
...  
Keyword(s):  
Antioxidant Activities ◽  
Ultrasound Assisted Extraction ◽  
Assisted Extraction ◽  
Seed Hull ◽  
Ultrasound Assisted ◽  
Perilla Seed

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

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