scholarly journals In Vitro Antiaging Analysis of Topical Pharmaceutical Preparation Containing Mixture of Strawberry Fruit, Pomelo Peel, and Langsat Fruit Extracts

2020 ◽  
pp. 53
Author(s):  
Endang Lukitaningsih ◽  
Anjar Hermadi Saputro ◽  
Mirna Widiasri ◽  
Nibras Khairunnisa ◽  
Nisrina Prabaswari ◽  
...  
Keyword(s):  
Pharmaceutical Preparation ◽  
Chemical Properties ◽  
Methyl Cellulose ◽  
Gelling Agent ◽  
Strawberry Fruit ◽  
Fruit Peel ◽  
Stability Parameters ◽  
Pomelo Peel ◽  
Thaw Cycle

The previous research has discovered that strawberry fruit, pomelo peel and langsat fruit peel have antioxidant activity. This research aimed to put the extract combination into several formula of gel and cream. Extract will be formulated into two gels with Natrium Carboxyl Methyl Cellulose as gelling agent for Formula 1 and Synthalen for Formula 2. Whereas there are three cream formulations with Glyceril Mono Stearat as surfactant for Formula 3, Polawax for Formula 4, and Simulsol 165 for Formula 5. Natrosol HBr was added to Formula 3 as thickening agent and Keltrol CG-SFT added to Formula 5. After five formulas being made, their stability was tested using climatic chamber within 30 days. Physical stability parameters were spreadability, stickiness, pH, viscosity, separation degree, and syneresis test. The chemical properties evaluation of the formula was done by measuring radical 2,2-difenyl-1-pikrylhidrazil (DPPH) scavenging activity percentage, anti-collagenase activity, anti-tyrosinase activity, and anti-elastase activity. The results showed that all of formulas have good activity in scavenging DPPH radical, anti-elastase, anti-collagenase and anti-tyrosinase as well. In addition, all formulas have good stability. There is no change in appearance after three times freeze-thaw cycle. Therefore, it was concluded that all formula can be developed as topical preparation for antiaging.

Levofloxacin loaded gelrite-cellulose polymer based sustained ocular drug delivery: formulation, optimization and biological study

2016 ◽  
Vol 36 (8) ◽  
pp. 761-769 ◽  
Author(s):  
Mohammed Aslam ◽  
Syed Sarim Imam ◽  
Mohammed Aqil ◽  
Yasmin Sultana ◽  
Asgar Ali
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Methyl Cellulose ◽  
Fickian Diffusion ◽  
Gelling Agent ◽  
Biological Study ◽  
Sterility Testing ◽  
Ocular Irritation

Abstract In the present work, levofloxacin in situ gel formulation was developed using gelrite as a gelling agent in combination with hydroxy propyl methyl cellulose. The developed formulations were evaluated for physicochemical parameters, in vitro release, ex vivo transcorneal study, sterility testing, antimicrobial efficacy, ocular irritation study, histopathological and stability evaluation. The in vitro drug release study showed the extended drug release up to 12 h, and the best fit kinetic model was found to be Peppas model (R2=0.9654), suggesting a Fickian diffusion process. The developed formulations showed optimized physicochemical results for all parameters. The optimized formulation showed therapeutically efficacious antimicrobial activity. Hens egg test-chorioallantoin membrane assay (HET-CAM) showed a mean score of 0.33 up to 24 h, which indicated the non-irritant property of the developed formulation. This non-irritant and stable in situ gel formulation of levofloxacin was found to be promising and safe for use as ocular delivery. The degradation rate constant and shelf life of developed optimized formulation (F14) were found to be low (1.213×10-4 at 25°C) and 2.14 years, respectively. This renders them favorable for ocular use as they would gel once in contact with the tear fluid, thus reducing nasolacrimal drainage, but would thin upon shearing, preventing ocular irritation and therefore induced lacrimation.

Design and Evaluation of Ion Activated In-Situ Ophthalmic Gel of Brimonidine Tartarate Using Kappa Carrageenan

2018 ◽  
Vol 8 (2) ◽  
Author(s):  
Vazir Ashfaq Ahmed ◽  
Divakar Goli
Keyword(s):  
Drug Release ◽  
Factorial Design ◽  
Chorioallantoic Membrane ◽  
Methyl Cellulose ◽  
Gelling Agent ◽  
Release Formulation ◽  
23 Factorial Design ◽  
Kappa Carrageenan

The objective of the study was to develop optimized formulation of In-situ gel of Brimonidine tartarate (BT), anti-glaucoma agent using Ion activated polymer; Gelrite as gelling agent, kappa carrageenan as mucoadhesive agent and Hydroxy Propyl Methyl Cellulose (HPMC E50) as release retardant polymer. The 23 factorial design was employed to optimize the formulation considering concentration of Gelrite, kappa carrageenan and Hydroxy Propyl Methyl Cellulose as independent variables, mucoadhesive force (N). Viscosity (cP) and In-vitro percentage drug release as dependent variables. Based on mucoadhesive force (N), Viscosity(CPS) and In-vitro percentage drug release, formulation containing concentration Gelrite (0.39%), kappa carrageenan (0.21%) and HPMC E50 (0.4%) was found to be optimized formulation developed by23 factorial design. Formulation was prepared successfully and assessed for gelling capacity, pH, rheological studies,refractive index, optical clarity, isotonicity and as ocular irriation by hen’s egg chorioallantoic membrane (HET-CAM) Test. The overall results of this study revealed that the Brimonidine tartarate/kappa carrageenan in-situ system can be used to enhance ocular retention time.

scholarly journals DESIGN AND EVALUATION OF GUANFACINE EXTENDED RELEASE FORMULATION

2019 ◽  
pp. 43-48
Author(s):  
SANJEEVANI DESAI ◽  
DURGACHARAN BHAGWAT ◽  
SUNITA SHINDE ◽  
JOHN DISOUZA
Keyword(s):  
Extended Release ◽  
In Vitro Release ◽  
Chemical Properties ◽  
Methyl Cellulose ◽  
Stability Study ◽  
Angle Of Repose ◽  
Content Uniformity ◽  
Release Formulation ◽  
Weight Variation

Objective: The present study was aimed to develop of the Guanfacine Hydrochloride Extended-release tablets for the treatment of Attention Deficit Hyperactivity Disorder (ADHD). The dosage regimen of Guanfacine Hydrochloride is 4 mg at every 6 h. The concentration of Guanfacine in plasma is fluctuating. Hence, to control the plasma fluctuation and to avoid toxicity problem, Guanfacine Hydrochloride was chosen as a drug with an aim to develop an extended release system for 20 to 24 h. Methods: The design of the system was based on the use of pH-dependent polymer (Hydroxypropyl Methyl Cellulose), pH-independent polymer (Eudragit L 100-55), along with microenvironment modifiers such as organic acid (Fumaric acid) were used in the formulation. Drug-excipient compatibility was studied by FTIR. Before compression, the granules were evaluated for precompression parameters such as bulk density, tapped density, an angle of repose, compressibility index and Hausner’s ratio. After compression, evaluation tests of tablets such as general appearance, hardness, thickness, weight variation, friability, content uniformity, in vitro release studies and stability studies were performed. Results: Out of 9 formulations, the drug release was found to be within the innovator formulation F9. The stability study of formulation F9 revealed there was no significant change in physical and chemical properties of drug stored at 40 °C/75 % RH, 30 °C/65 % RH, 25 °C/60 % RH for 2 mo. Conclusion: Optimized formulation batch F9 showed highest F2 value which indicates similarity with innovator product. The study indicates that Guanfacine Hydrochloride Extended-release tablet was successfully developed.

scholarly journals Development and Evaluation of Indomethacin Controlled Release Press Coated Tablets

2016 ◽  
Vol 14 (2) ◽  
pp. 187-192
Author(s):  
Muhammad Rashedul Islam ◽  
Md Elias Al Mamun ◽  
Md Mizanur Rahman Moghal ◽  
Md Habibur Rahman
Keyword(s):  
Drug Release ◽  
Xanthan Gum ◽  
Chemical Properties ◽  
Methyl Cellulose ◽  
Compression Pressure ◽  
Physico Chemical ◽  
Compression Coating ◽  
Coating Formulation ◽  
Coating Formulations

In the present work, several batches of indomethacin press coated tablets were prepared with drug and Avicel PH 102 utilizing the press coating technology. The core tablet was compression coated with minimal compression pressure. The compression coating mixture was formulated using various amount of lactose and xanthan gum which was used as the release retarding agent. Three formulations (IX-1, IX-2 and IX-3) were designed to evaluate the release profile as function of xanthan gum load. In vitro drug release testing demonstrated that the drug release was inversely proportional to the amount of xanthan gum in the coating formulations. In addition, formulation IX-2 was modified by incorporating hydroxypropyl methyl cellulose (HPMC) 15 cps into the compression coating formulation to understand their effects on drug release. The formulation was evaluated for its properties and correlated with in vitro and kinetic release studies. Incorporation of HPMC caused the highest fraction of drug to be released in the dissolution fluid. The physico-chemical properties of the excipients can be held responsible for the discrepancy in release rate of indomethacin. From kinetic analysis drug release was found to follow Higuchi mechanism for all the formulations. Overall, the study concluded that excipients present in the coating formulations make a significant impact on drug release.Dhaka Univ. J. Pharm. Sci. 14(2): 187-192, 2015 (December)

Formulation and In vitro Release Characterization of Metoprolol Succinate Extended Release Tablets

2012 ◽  
Vol 4 (4) ◽  
pp. 1537-1543
Author(s):  
Sakthikumar T ◽  
Rajendran N N ◽  
Natarajan R
Keyword(s):  
Drug Release ◽  
Extended Release ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Wet Granulation ◽  
Direct Compression ◽  
Metoprolol Succinate ◽  
Extended Release Formulations ◽  
Vitro Release

The present study was aimed to develop an extended release tablet of metoprolol Succinate for the treatment of hypertension.  Four extended release formulations F1-F4 were developed using varying proportions of hydroxylpropyl-methylcellulose K100M, sodium carboxy methyl cellulose and Eudragit L30 D55 by wet granulation. Five extended release formulations F5-F9 containing HPMC K100M and HPMC 5 cps in varying concentration were developed by direct compression. The physicochemical and in vitro release characteristics of all the formulations were investigated and compared. Two formulations, F7 and F8 have shown not more 25% drug release  in 1st h, 20%-40% drug release at 4th hour, 40%-60% drug release at 8th hour and not less than 80% at 20th hour and the release pattern conform with USP specification for 24 hours extended release formulation. It can be conclusively stated that optimum concentration of HPMC K100M (58%-65%) by direct compression method can yield an extended release of metoprolol succinate for 24 hours.

Development and Ex-vivo Evaluation of Topiramate Mucoadhesive Nanoparticles for Intranasal Delivery

2020 ◽  
Vol 13 (6) ◽  
pp. 5250-5255
Author(s):  
Ashwin Kumar Tulasi ◽  
Anil Goud Kandhula ◽  
Ravi Krishna Velupula
Keyword(s):  
Particle Size ◽  
Nasal Mucosa ◽  
Intranasal Administration ◽  
Ex Vivo ◽  
Chemical Properties ◽  
Brain Targeting ◽  
Oral Tablet ◽  
Promising Alternative ◽  
Ex Vivo Permeation

Topiramate is a second-generation antiepileptic drug used in partial, generalized seizures as an oral tablet. Oral route of administration is most convenient but shows delayed absorption. Moreover, in emergency cases, parenteral administration is not possible as it requires medical assistance. Hence, the present study was aimed to develop topiramate mucoadhesive nanoparticles for intranasal administration using ionotropic gelation method. The developed nanoparticles were evaluated for physico-chemical properties like particle size, zeta potential, surface morphology, drug content, entrapment efficiency, in vitro drug release, mucoadhesive strength, and ex vivo permeation studies in excised porcine nasal mucosa. Optimized nanoparticle formulation (T9) was composed oil mucoadhesive agent (Chitosan 1% w/w), cross linking polymer (TPP) and topiramate 275mg, 100mg and 4% respectively. It showed particle size of 350nm, high encapsulation efficacy and strong mucoadhesive strength. In vitro drug diffusion of optimized formulation showed 95.12% release of drug after 180min. Ex-vivo permeation of drug across nasal mucosa was   88.05 % after 180min. Nasocilial toxicity studies showed optimized formulation did not damage the nasal mucosa. Thus, the intranasal administration of topiramate using chitosan can be a promising alternative for brain targeting and the treatment of epilepsy.

scholarly journals FORMULATION AND IN VITRO, IN VIVO EVALUATION OF PRONIOSOMAL GEL OF NEOMYCIN SULPHATE

2019 ◽  
pp. 156-163
Author(s):  
AMOL SHETE ◽  
PRIYANKA THORAT ◽  
RAJENDRA DOIJAD ◽  
SACHIN SAJANE
Keyword(s):  
Phase Separation ◽  
Skin Irritation ◽  
Entrapment Efficiency ◽  
Separation Method ◽  
Gelling Agent ◽  
In Vivo Evaluation ◽  
Skin Delivery ◽  
Span 60

Objective: The objectives of present investigation were to prepare and evaluate proniosomes of neomycin sulphate (NS) by coacervation phase separation method by using sorbitan monostearate (span 60) and lecithin as a surfactant to increase the penetration through the skin and study the effect of concentration of the same. Methods: Proniosomes of neomycin sulphate (NS) were prepared by coacervation phase separation method by using span 60 and lecithin. The effect of concentration of span 60 and lecithin was studied by factorial design. The prepared proniosomes were converted to gel by using carbopol as a gelling agent. The prepared formulations were evaluated for entrapment efficiency, in vitro drug diffusion, in vitro antibacterial activity and in vivo skin irritation test etc. Results: All Formulation showed the percentage entrapment efficiency in the range 38.31±0.05% to 77.96±0.06%, good homogeneity and gel was easily spreadable with minimal of shear. Optimized formulation showed enhanced rate of diffusion in vitro, increase in zone of inhibition against staphylococcus aureus, no skin irritation and showed good stability. Conclusion: The results of present study indicates that proniosomal gel formulated by using combination of span 60, Lecithin, cholesterol can be used to enhance skin delivery of NS because of excellent permeation of drug. Developed proniosomal gel formulation was promising carrier for NS

scholarly journals Lignans of Sesame (Sesamum indicum L.): A Comprehensive Review

Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 883
Author(s):  
Mebeaselassie Andargie ◽  
Maria Vinas ◽  
Anna Rathgeb ◽  
Evelyn Möller ◽  
Petr Karlovsky
Keyword(s):  
Biological Activities ◽  
Chemical Properties ◽  
Transformation Products ◽  
Extensive Literature ◽  
Controversial Issues ◽  
Sesame Seeds ◽  
Historical Texts ◽  
Health Promoting ◽  
Processed Products

Major lignans of sesame sesamin and sesamolin are benzodioxol--substituted furofurans. Sesamol, sesaminol, its epimers, and episesamin are transformation products found in processed products. Synthetic routes to all lignans are known but only sesamol is synthesized industrially. Biosynthesis of furofuran lignans begins with the dimerization of coniferyl alcohol, followed by the formation of dioxoles, oxidation, and glycosylation. Most genes of the lignan pathway in sesame have been identified but the inheritance of lignan content is poorly understood. Health-promoting properties make lignans attractive components of functional food. Lignans enhance the efficiency of insecticides and possess antifeedant activity, but their biological function in plants remains hypothetical. In this work, extensive literature including historical texts is reviewed, controversial issues are critically examined, and errors perpetuated in literature are corrected. The following aspects are covered: chemical properties and transformations of lignans; analysis, purification, and total synthesis; occurrence in Seseamum indicum and related plants; biosynthesis and genetics; biological activities; health-promoting properties; and biological functions. Finally, the improvement of lignan content in sesame seeds by breeding and biotechnology and the potential of hairy roots for manufacturing lignans in vitro are outlined.

scholarly journals Survey of Phenolic Acids, Flavonoids and In Vitro Antioxidant Potency Between Fig Peels and Pulps: Chemical and Chemometric Approach

Molecules ◽  
2021 ◽  
Vol 26 (9) ◽  
pp. 2574
Author(s):  
Lahcen Hssaini ◽  
Francisca Hernandez ◽  
Manuel Viuda-Martos ◽  
Jamal Charafi ◽  
Rachid Razouk ◽  
...  
Keyword(s):  
Phenolic Acids ◽  
Radical Scavenging ◽  
Fruit Peel ◽  
Mean Values ◽  
Local Cultivar ◽  
Ic50 Values ◽  
The Mean ◽  
Lipid Peroxidation Inhibition ◽  
Almost All

In the present study, chromatic coordinates, phenolic acids, flavonoids and antioxidant capacity assessed by 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2′-azino-bis (3-ethylbenzothiazoline-6-sulfonate (ABTS) and lipid peroxidation inhibition capacity (LPIC) essays and their relative IC50 were investigated in 25 fig cultivars growing in Morocco. The aims of this study were to determine (i) the variation in these compounds among light and dark-colored cultivars, (ii) their partitioning between fruit peel and pulp and (iii) to display network connections among these variables. Twelve phenolic compounds (PCs) were isolated in peel extract versus eight in pulp samples. Anthocyanins, mainly cyanidin-3,5-diglucoside and cyanidin-3-O-rutinoside, were the predominant compounds in peels, where the mean concentrations were 75.90 ± 18.76 and 77.97 ± 18.95 µg/g dw, respectively. On the other hand, (−)-epicatechin and cyanidin-3-O-rutinoside were the major compounds in the pulp extracts, where the mean values were 5.23 ± 4.03 and 9.01 ± 5.67 µg/g dw, respectively. A two-dimensional hierarchically clustered heatmap was applied to the dataset to explore correlations in the dataset and similarities between cultivars, without dimensionality reduction. Results showed that anthocyanins, particularly pelargonidin-3-O-rutinoside, cyanidin-3,5-diglucoside and cyanidin-3-O-rutinoside, were the main contributors to the peels’ free radical scavenging capacity. This capacity was particularly higher in the peel of dark-colored figs compared to the fruit pulp. The local cultivar “INRA 1301” showed the most promising phenolic profile due to its very high levels of almost all detected PCs, especially (−)-epicatechin, quercetin-3-O-rutinoside, quercetin-3-O-glucoside, cyanidine-3,5-diglucoside, cyanidine-3-O-rutinoside and pelargonidin-3-O-rutinoside (54.66, 141.08, 35.48, 494.08, 478.66, 12.56 µg/g dw, respectively). Having the darkest figs in the collection (L* = 25.72, c* = 22.09 and h° = 20.99), this cultivar has also combined promising IC50 values, which were of 19.85, 40.58 and 124.78 µg/mL for DPPH, ABTS and LPIC essays, respectively.

scholarly journals Evaluation of antipsoriatic activity of gel containing Pongamia pinnata extract on Imiquimod-induced psoriasis

2021 ◽  
Vol 7 (1) ◽  
Author(s):  
Kamlesh Wadher ◽  
Shital Dabre ◽  
Anjali Gaidhane ◽  
Sagar Trivedi ◽  
Milind Umekar
Keyword(s):  
Mouse Model ◽  
Pongamia Pinnata ◽  
Gelling Agent ◽  
Proper Treatment ◽  
Phytochemical Screening ◽  
Diffusion Studies ◽  
In Vitro Diffusion ◽  
Gel Formulations ◽  
Disease And Disorders

Abstract Background Pongamia pinnata (Fabaceae) is among those categories of plants mentioned in Ayurveda and traditionally known to use in several types of disease and disorders. The objective of the present work was to investigate the anti-psoriatic activity of Pongamia pinnata leaves extracts in Herbal gel formulation. Results Hydroalcoholic leaves extract of Pongamia pinnata was first subjected to phytochemical screening and quantification of phytoconstituents. Herbal gel was prepared containing Pongamia pinnata extracts using Carbopol 934 as gelling agent. The prepared gel formulations were studied for pH, viscosity, Spreadability and in vitro diffusion studies. The imiquimod-induced psoriatic mouse model, showed a prominent anti-psoriatic activity of the extract as evident through index grading. Treatment with extract confirmed a noteworthy reduction in psoriasis in the treated groups as there was a considerable diminution in the thickness and scaling of skin. Conclusions Lack of proper treatment and disadvantages associated with allopathic medicines pave the way to extensive research in natural products with anti-psoriatic activity. The present research scientifically justified the anti-psoriatic activity of the Hydroalcoholic extracts of Pongamia pinnata leaves.

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