Chlorpromazine bioavailability from a topical gel formulation in volunteers

2013 ◽  
Vol 11 (3) ◽  
pp. 144-148 ◽  
Author(s):  
Amanda Weiland ◽  
Bridget Protus ◽  
Jason Kimbrel ◽  
Phyllis Grauer ◽  
Jennifer Hirsh
Keyword(s):  
2017 ◽  
Vol 2 (3) ◽  

Melanoma is the most dangerous type of skin cancer in which mostly damaged unpaired DNA starts mutating abnormally and staged an unprecedented proliferation of epithelial skin to form a malignant tumor. In epidemics of skin, pigment-forming melanocytes of basal cells start depleting and form uneven black or brown moles. Melanoma can further spread all over the body parts and could become hard to detect. In USA Melanoma kills an estimated 10,130 people annually. This challenge can be succumbed by using the certain anti-cancer drug. In this study design, cyclophosphamide were used as a model drug. But it has own limitation like mild to moderate use may cause severe cytopenia, hemorrhagic cystitis, neutropenia, alopecia and GI disturbance. This is a promising challenge, which is caused due to the increasing in plasma drug concentration above therapeutic level and due to no rate limiting steps involved in formulation design. In this study, we tried to modify drug release up to threefold and extended the release of drug by preparing and designing niosome based topical gel. In the presence of Dichloromethane, Span60 and cholesterol, the initial niosomes were prepared using vacuum evaporator. The optimum percentage drug entrapment efficacy, zeta potential, particle size was found to be 72.16%, 6.19mV, 1.67µm.Prepared niosomes were further characterized using TEM analyzer. The optimum batch of niosomes was selected and incorporated into topical gel preparation. Cold inversion method and Poloxamer -188 and HPMC as core polymers, were used to prepare cyclophosphamide niosome based topical gel. The formula was designed using Design expert 7.0.0 software and Box-Behnken Design model was selected. Almost all the evaluation parameters were studied and reported. The MTT shows good % cell growth inhibition by prepared niosome based gel against of A375 cell line. The drug release was extended up to 20th hours. Further as per ICH Q1A (R2), guideline 6 month stability studies were performed. The results were satisfactory and indicating a good formulation approach design was achieved for Melanoma treatment.


2017 ◽  
Vol 1 ◽  
pp. s57
Author(s):  
Sinyoung Jeong ◽  
Maiko Hermsmeier ◽  
Sam Osseiran ◽  
Akira Yamamoto ◽  
Usha Nagavarapu ◽  
...  

Abstract Not AvailableStudy supported by BioPharmX.


2020 ◽  
Vol 21 (15) ◽  
pp. 1699-1710
Author(s):  
Sonsawan Kongpuckdee ◽  
Suwipa Ungphaiboon ◽  
Supreedee Sungkharak ◽  
Narubodee Phadoongsombut ◽  
Sirima Mahattanadul

Background: Oral inflammatory ulcers are one of the common complaints of patients attending out-patient clinics. Previous in vivo studies had shown that an Aqueous M. citrifolia Fruit Extract (AMFE) possessed anti-inflammatory and ulcer healing activities. Therefore, a standardized topical bioadhesive gel containing AMFE-phytosome was developed and determined for its oral ulcer healing efficacy in a rabbit model. Methods: The AMFE phytosome (AMFE-P) was prepared by a complexation method with the required amount of AMFE: Phosphatidylcholine: Tween 80 to weigh ratio of 2:1:0.2. Poloxamer 407 was used as a gelling agent. The oral ulcer was induced in male New Zealand white rabbits by topical application of acetic acid. Each test compound was applied to the ulcer for 10 days beginning on the second day after the ulcer induction. Complete ulcer healing on the specimen obtained on day 12 was observed histologically using the histological scoring protocol. Results: The optimized gel containing AMFE-P equivalent to AMFE 10%w/w (10%AMFE-P gel) showed the best bioadhesive gel quality, a smooth and homogeneous texture with an optimum viscosity and pH range used in human oral cavity, a good physical and chemical stability and the highest percentage cumulative release of total phenolic and scopoletin content. It was found that a daily application of 10% AMFE-P gel exerted a superior ulcer healing efficacy and a significantly rapid ulcer healing process than a twice daily application of topical gel containing AMFE 10%w/w or chlorhexidine 0.2%. Conclusion: These findings demonstrated that 10% AMFE-P gel has potential as a safe and effective alternative therapeutic agent for oral ulcers.


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.


2021 ◽  
Vol 14 (1) ◽  
Author(s):  
Ali Pouryousef ◽  
Erfan Eslami ◽  
Sepehr Shahriarirad ◽  
Sina Zoghi ◽  
Mehdi Emami ◽  
...  

Abstract Objectives The current study aimed to evaluate the effects of Ficus carica latex on the treatment of cutaneous leishmaniasis (CL), induced by Leishmania major. A 5% topical gel with F. carica latex was prepared. BALB/c mice were infected by inoculation of amastigotes form of L. major. Thirty BALB/c mice were divided into five groups, where the first group was treated daily, the second group twice per day, and the third group every other day with the 5% topical gel, for 3 weeks. The sizes of the lesions were measured before and during the course of treatment. Results Although the mean size of lesions in the mice group treated with the 5% F. carica gel, especially in the group receiving daily treatment, was less than the mean size of the lesions in the control group, yet, the differences was not statistically significant (p > 0.05). The findings of the current study demonstrated that the 5% F. carica latex with a 3-week course of treatment had no considerable effect in recovery or control of CL induced by L. major in the murine model. Using higher concentration of F. carica latex and with longer treatment lengths may increase its efficacy in the treatment of CL.


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