A novel plaster containing benzoyl peroxide microsponges: Formulation, development and evaluation

2020 ◽  
pp. 152808372098046
Author(s):  
Nihal Atabay ◽  
Ayse Merih Sariişik ◽  
Sinem Yaprak Karavana ◽  
Seda Rençber

Benzoyl peroxide is a widely used active agent for acne vulgaris treatment that has antibacterial, anti-inflammatory, keratolytic and wound-healing properties. The common complaints for benzoyl peroxide are skin irritation and dryness. To reduce these side effects, microsponge formulations are used as an effective tool in pharmaceutical and cosmetic industries. In this study, a medical plaster was developed containing benzoyl peroxide microsponges which gives an opportunity to explore the potential of the microsponge systems in textile industry. Benzoyl peroxide microsponge was obtained by using quasi-emulsion solvent diffusion method and characterized by SEM, FT-IR, particle size analysis and porosity studies. The microsponges were applied onto 100% cotton woven fabric by using dip-coating technique. In the treatment solution, different binding agents as acrylic binder, and cross-linking agents as poly(ethylene glycol) diglycidyl ether and 1,2,3,4-butanetetracarboxylic acid were used. Microsponges were around 78.4 µm in diameter and had a spherical porous surface. SEM analyses of the treated fabrics proved that the microsponges were succesfully transferred on cotton fabrics. The drug contents of the fabrics containing Benzoyl peroxide loaded microsponge were found to be within the range of 68.512–102.873%. The in vitro drug release results show that the release from both samples was more than 40% within 6 h. The water vapor permeability of plaster prepared with acrylic binder (S1) was significantly higher than the other plasters. This study presents a novel approach for acne treatment based on textiles containing microsponges. The results revealed that microsponges had a promising potential in textile field.

Author(s):  
Shreya Nikam

Objective: Isotretinoin is a very effective drug in the treatment of acne vulgaris by topically. The objective of present study was formulation development of anti-acne gel using Isotretinoine and span 80 for topical delivery to cure nodulosystic acne vulgaris. Furthermore, the comparative study of all the evaluation parameters done with marketed formulation of same drug.Methods: Formulation of anti-acne gel of isotretinoin using Carbopol 940 as a polymer and incorporating isotretinoin in form of topical semi-solid gel using magnetic stirrer, Cremophor RH 40, and butylated hydroxytoluene. Drug was uniformly dispersed in Cremophor RH 40 and the respected solvents. Ethanol, isopropyl alcohol, and glycerin were used as solvents in 15% quantity. Further, the formulation was evaluated for physicochemical evaluation of gel formulations. The prepared gel were optimized statistically and characterized for pH, spredability, drug content, viscosity, in vitro diffusion study, acute skin irritation test, and antimicrobial activity. Evaluation test was also compared with marketed formulation of isotretinoin, that is, Sortet gel. The antibacterial and anti-acne activity of different formulations was determined by modified agar well diffusion method on the culture of Propionibacterium acne also compared with marketed formulation.Results: The optimized batch (B10) showed highest spreadability (32.422 g/cm3) in all formulations and also have high percentage of drug contents (95.60%). The spreadability value was 17.998 g/cm3 showing good spreadability. The viscosity of optimized batch was observed less as compared to other formulations, ultimately showed releases also more. In the in vitro diffusion study, B10 batch release 85.69% of the drug as compared to Sotret gel. The antibacterial activity was studied on anaerobic microorganism P. acne, compared with marketed Sortet gel. Optimized batch showed maximum zone of inhibition to P. acne below marketed formulations and standard benzyl peroxide gel.Conclusion: The topical anti-acne gel of isotertinoin was successfully formulated and evaluated for different parameters. The results indicate that the active component, that is, isotertinoin is more effective when subjected in gel formulations and produces effective anti-acne activity in the management of nodulosystic acne vulgaris.


2019 ◽  
Vol 9 (3) ◽  
pp. 222-233
Author(s):  
Divya D. Jain ◽  
Namita D. Desai

Background: Adapalene is a promising third generation retinoid used in the topical treatment of acne vulgaris. However, the major drawback associated with conventional topical therapy of Adapalene is the ‘retinoid reaction’ which is dose-dependent and characterized by erythema, scaling and burning sensation at the application sites. Microparticulate drug delivery can play a major role in reducing side effects and providing better patient compliance due to targeted delivery. Methods: Adapalene microparticles were prepared using quasi emulsion solvent diffusion method. The effects of formulation variables including polymer ratios, amounts of emulsifier, drug loading and process variables such as stirring time and speed on the physical characteristics of microparticles were investigated. The developed microparticles were characterized by DSC and SEM. Adapalene microparticles were incorporated into Carbopol 971 NF gel for ease of topical delivery. Results: Adapalene microparticulate topical gel showed sustained drug release over 8 hours in in vitro studies. The amount of drug retained in the rat skin during ex vivo studies was higher in the microparticulate topical gel (227.43 ± 0.83 µg/cm2) as compared to the marketed formulation (81.4 ± 1.11 µg/cm2) after 8 hours indicating localized and sustained drug action that can be useful in treating acne vulgaris. The safety of optimized Adapalene gel determined by skin irritation studies performed on Sprague Dawley rats showed no irritation potential. Conclusion: Microparticles can provide promising carrier systems to deliver Adapalene, improving patient compliance due to enhanced skin deposition, localized and sustained action with reduced associated irritant effects.


2020 ◽  
Vol 10 (6) ◽  
pp. 74-85
Author(s):  
Sonali Syal ◽  
Vinay Pandit ◽  
Amar Deep Ankalgi ◽  
C.P.S Verma ◽  
M.S. Ashawat

The aim of this study was to develop the Microsponges containing Havan ash composed gel formulation for the treatment of Acne. Therefore, the topical formulation containing microsponges of Havan Ash will be formulated and evaluated. The preliminary investigation was carried out for the formulation of Havan ash loaded Microsponges by using quasi emulsion solvent diffusion method (MSF1-MSF6). In the preformulation studies of Havan ash the physical description and organoleptic properties, pH, acid insoluble ash, water-soluble ash, IR spectroscopy, identification test, rheological study, atomic absorption spectroscopy is also carried out. On the basis of particle size analysis of Microsponges, percentage yield formulation MSF5 containing Microsponges formula was selected for composition of topical gel formulation. Thus the different gel base formulation (G1-G3) using Carbopol-934 (1,1.5,2.0%) was prepared by emulsification method. By considering all the relevant, physicochemical parameters, G2 gel base was selected for further loading of Havan ash containing Microsponges. The MSF5 formulation was loaded into the selected gel base G2 (1.5%). Then the formulation and evaluation of Havan ash microsponges loaded gel was done. The formulation F3 has better results than other 4 formulations. F3 have its appearance silver colour, consistency very good, Grittiness –ve, homogeneity good, wash ability very good, pH 6.3, Spreadabilty (g.cm/sec) 14.4 ± 0.77 7and viscosity (cps) 18251 ± 50.12, have good result of psychometric analysis. With the revealed results by different evaluation parameters, it is concluded that microsponges drug delivery system has become highly competitive and rapidly evolving technology and more research are carrying out to optimize cost-effectiveness and efficacy of the therapy. Keywords: Havan ash, Antimicrobial, Microsponges, Acne vulgaris, Topical gel.


Molecules ◽  
2020 ◽  
Vol 25 (20) ◽  
pp. 4856
Author(s):  
Liza Józsa ◽  
Zoltán Ujhelyi ◽  
Gábor Vasvári ◽  
Dávid Sinka ◽  
Dániel Nemes ◽  
...  

Natural products used in the treatment of acne vulgaris may be promising alternative therapies with fewer side effects and without antibiotic resistance. The objective of this study was to formulate creams containing Spirulina (Arthrospira) platensis to be used in acne therapy. Spirulina platensis belongs to the group of micro algae and contains valuable active ingredients. The aim was to select the appropriate nonionic surfactants for the formulations in order to enhance the diffusion of the active substance and to certify the antioxidant and antibacterial activity of Spirulina platensis-containing creams. Lyophilized Spirulina platensis powder (SPP) was dissolved in Transcutol HP (TC) and different types of nonionic surfactants (Polysorbate 60 (P60), Cremophor A6:A25 (CR) (1:1), Tefose 63 (TFS), or sucrose ester SP 70 (SP70)) were incorporated in creams as emulsifying agents. The drug release was evaluated by the Franz diffusion method and biocompatibility was tested on HaCaT cells. In vitro antioxidant assays were also performed, and superoxide dismutase (SOD) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) assays were executed. Antimicrobial activities of the selected compositions were checked against Staphylococcus aureus (S. aureus) and Cutibacteriumacnes (C. acnes) (formerly Propionibacterium acnes) with the broth microdilution method. Formulations containing SP 70 surfactant with TC showed the most favorable dissolution profiles and were found to be nontoxic. This composition also showed significant increase in free radical scavenger activity compared to the blank sample and the highest SOD enzyme activity was also detected after treatment with the cream samples. In antibacterial studies, significant differences were observed between the treated and control groups after an incubation time of 6 h.


2021 ◽  
Vol 8 (10) ◽  
pp. 440-457
Author(s):  
Ponni Sujathan ◽  
Umesh Kumar Sharma

The objective of present work was formulation and evaluation of Metronidazole loaded microsponges for the management of diabetic foot ulcer via topical application and to reduce side effects. The microsponges were prepared by quasi-emulsion solvent diffusion method using different concentrations of Ethyl cellulose and Poly vinyl alcohol. The prepared microsponges were evaluated for particle size analysis, SEM, % production yield, % drug entrapment efficiency, in-vitro drug release studies, DSC and antimicrobial studies. FTIR studies shown that there was no interaction between drug and polymers. The optimum sustained release of drug around a period of 12hrs was shown by formulation F8. The n value of optimized formulation indicated that the drug release followed zero order kinetics. It was confirmed from the stability studies that the optimized formulation remained stable at 45±2℃ and 70±5% relative humidity. Keywords: Microsponges, Metronidazole, Diabetic Foot, Quasi-emulsion solvent diffusion, Sustained release, Scanning electron microscopy, Differential scanning calorimetry.


2016 ◽  
Vol 62 (2) ◽  
pp. 3-16 ◽  
Author(s):  
Nadica Sibinovska ◽  
Venera Komoni ◽  
Katerina Ancevska Netkovska ◽  
Edina Vranic ◽  
Maja Simonoska Crcarevska ◽  
...  

Acne vulgaris (acne) is chronic inflammatory dermatosis which affects the pilosebaceous unit, with a varied clinical picture including inflammatory and non-inflammatory cutaneous lessions. This multifactorial disease mostly occurs in adolescents; however, it can also affect children and adults. Different therapy options for acne treatment exist, comprising topical, systemic and hormonal agents or a combination thereof. The choice of the therapy depends on various factors, for instance the severity and extent of the disease and site of involvement. Commonly used topical acne therapies include benzoyl peroxide, salicylic acid, antibiotics, retinoids, azelaic acid, sulfone agents and their combinations. Systemic antibiotics are indicated for use in moderate to severe inflammatory acne and should be used in combination with a topical retinoid and benzoyl peroxide. The available conventional formulations often cause side effects such as skin irritation, dryness, peeling, itching, leading to reduced patient compliance and compromised therapeutical efficacy. Novel drug delivery systems are promising option for improved acne treatment outcome, as they can diminish the side effects caused by the therapeutic agents or can modulate their properties and at the same time offering possibilities for modified release and improved skin penetration of the active substances. The cosmetics manufacturers implement micro/nanotechnology in their formulations, while patent protection for cosmetics has gained more importance over the past decades. This review focuses on micro/nanoparticulated carrier systems that can be used for acne treatment and the published patents concerning them.


2020 ◽  
Vol 21 (4) ◽  
pp. 341-351
Author(s):  
Ruchi Sharma ◽  
Nitish Kumar ◽  
Sompal P. Singh ◽  
Sunil Kumar ◽  
Rekha Rao

Background: Citronella Oil (CO) was used by the Indian army as mosquito repellant to repel mosquitoes at the beginning of the 20th century and later in 1948, it was registered in the USA for commercial purposes. Due to its ecofriendly nature, CO possesses immense potential as a mosquito repellent. Methods: Citronella oil is a valuable alternative to synthetic mosquito repellents commonly used nowadays. However, its volatile nature, poor stability in air and high temperature restrict its application. Its direct application on skin may lead to skin irritation. To surmount the above-mentioned issues, the present research aims to develop Microsponge (MS), a novel dosage form for enhancing the utility and safety of CO. Quasi emulsion solvent diffusion method was chosen for crafting MS using ethyl cellulose with various drug-polymer ratios and characterized. In vitro cytotoxicity evaluation was also carried out to check the dermal safety of COMS. Results: The present results revealed that the size of all prepared formulation lies in the micro range (20 ± 3 to 41 ± 4 μm), with good payload (42.09± 3.24 to 67.08± 6.43%). The results of FE-SEM depicted that MS were spherical in shape with porous nature. Cytotoxicity results indicated that COMS were safe on skin cells, when compared to pure CO. The optimized MS were also assessed for larvicidal assay against larvae of Anopheles culicifacies. Conclusion: The CO micro-formulations were found to possess enhanced stability of this oil. Entrapment of CO in MS resulted in a better vehicle system in terms of safety, stability and handling benefits of this oil.


2020 ◽  
Vol 14 (2) ◽  
pp. 145-161
Author(s):  
Mankaran Singh ◽  
Deepak Sharma ◽  
Dinesh Kumar ◽  
Gurmeet Singh ◽  
Gaurav Swami ◽  
...  

Background: Dental caries originate due to the localized dissolution of the hard tissues of teeth, mainly caused by acids, developed by the presence of microorganisms in the biofilm (dental plaque) on the surface of teeth causing “cavities”. Commercially available liquid mouthwashes containing synthetic active ingredients possess limitations like teeth staining, higher alcoholic content, taste disturbances, xerostomia, and stability issues. Objective: To make the solid preparation for oral hygiene (US6428770B1) in the form of herbal effervescent mouthwash tablet (CN106619318A, US8728446B2) using Azadirachta indica and Curcumin having antimicrobial, antibacterial, antiplaque, and anti-inflammatory activity. Methods: The optimization study of effervescent granules was performed by 33 factorial design. A total of 27 preliminary experimental batches were prepared by the fusion method, varying the amount of citric acid, tartaric acid, and sodium bicarbonate. A complex of curcumin was prepared with hydroxyl propyl β-cyclodextrin and further examined by scanning electron microscopy. The prepared tablets were evaluated for pre and post-compression parameters. The in vitro antimicrobial study was performed by Agar well diffusion method against S. mutans. Results: All the experimental batches of effervescent granules were evaluated for pH, effervescent time, and CO2 content. Six batches were further selected for final tablet preparation. The results of the pre-compression parameters revealed excellent flow properties and post-compression parameters; the results were also significant. The antimicrobial study revealed the F3 as a final best formulation. Conclusion: The developed herbal formulation (F3) has a good potential to maintain oral hygiene as compared to alcoholic mouthwash and further studies may be necessary to confirm the efficacy of the formulation since only a single bacterial strain was assayed.


Cosmetics ◽  
2020 ◽  
Vol 7 (3) ◽  
pp. 70 ◽  
Author(s):  
Muhammed Majeed ◽  
Shaheen Majeed ◽  
Kalyanam Nagabhushanam ◽  
Lakshmi Mundkur ◽  
H. R. Rajalakshmi ◽  
...  

Acne vulgaris is a common skin disorder of pilosebaceous units. The therapy for mild-to-moderate acne includes topical antibiotics, benzoyl peroxide and retinoids. In this open-label, randomized monocentric study, we compared the efficacy of LactoSporin® 2% w/w cream with benzoyl peroxide in 64 male and female subjects with mild-to-moderate acne for three weeks. The efficacy parameters were evaluated based on the dermatologist visual assessment and instrumental measurements using Sebumeter® MPA580, Antera 3DTM and VISIA CR 2.2 and subject self-assessment questionnaires. Adverse events were recorded throughout the study period. In order to understand the mechanism of action and properties of LactoSporin, the pH stability, thermostability, antimicrobial activity and 5-alpha reductase activity were evaluated in vitro. A significant improvement was observed in the dermatological assessment of closed comedones (p < 0.0001), open comedones (p = 0.0069) and papules count (p < 0.0001) in comparison to the baseline in both LactoSporin and benzoyl peroxide groups. The antera analysis showed significant improvement in redness (p < 0.0001) and elevation (p < 0.0001) (small and medium) in both the treatment groups. The sebumeter analysis showed a significant decrease in sebaceous secretion (p < 0.0001) for LactoSporin, which resulted in reduced oiliness, pimples, acne spots and redness around the acne spot. The product was found to be safe without any irritancy. LactoSporin was stable at an acidic pH and temperature range of 70 to 90 °C, with antimicrobial activity against various pathogenic bacteria, including Cutibacterium acnes. It was also a potent inhibitor of 5-alpha reductase activity. Thus, it can be concluded that the efficacy of LactoSporin is equivalent to benzoyl peroxide in the treatment of mild-to-moderate acne lesions and better than benzoyl peroxide for reducing the sebaceous secretion and oily, greasy nature of the skin, implying its efficacy in other sebohorriec conditions.


2018 ◽  
Vol 6 (2) ◽  
pp. 52-58
Author(s):  
Bikram Gautam ◽  
Elisa Dongol ◽  
Anima Shrestha

Background: Tooth brushing with toothpaste is the most widely practiced form of oral hygiene. Toothpaste aids to improve oral hygiene and effective plaque removal. A wide range of chemicals, mainly antimicrobial agents, have been added to toothpastes which kill microorganisms by disrupting their cell walls and inhibiting their enzymatic activity.Objectives: The aim of the study was to determine the antimicrobial activity of toothpastes.Methods: Eight (Two herbal and six regular) toothpastes were selected for the study. The study was conducted from October to November 2016 at St. Xavier’s College’s microbiology laboratory. Antimicrobial activity of toothpastes were assessed by measuring inhibition zones by broth dilution method and agar well diffusion method.Results: Minimum Inhibitory Concentration determination by tube dilution method and cup well diffusion method was found to be same. The antimicrobial activity on test organisms was shown by all toothpastes (TH1, TH2, TR3, TR4, TR5, TR6, TR7 and TR8). Antimicrobial activity of all toothpastes were almost the same and was statistically significant (t>0.05)Conclusion: All eight toothpastes aids in lower microbial load. However, no toothpaste showed bactericidal and fungicidal effect against the tested microbes. The toothpaste containing only natural active ingredients were found to be more effective than the toothpaste containing chemical active agent followed by weaker antimicrobial effect given by the toothpaste containing both natural and chemical active ingredient as an antimicrobial agent.


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