scholarly journals Influence of Bile Acids in Hydrogel Pharmaceutical Formulations on Dissolution Rate and Permeation of Clindamycin Hydrochloride

Gels ◽  
2022 ◽  
Vol 8 (1) ◽  
pp. 35
Author(s):  
Nebojša Pavlović ◽  
Isidora Anastasija Bogićević ◽  
Dragana Zaklan ◽  
Maja Đanić ◽  
Svetlana Goločorbin-Kon ◽  
...  
Keyword(s):  
Bile Acids ◽  
Cholic Acid ◽  
Skin Penetration ◽  
Pharmaceutical Formulations ◽  
Penetration Enhancers ◽  
Gelling Agent ◽  
Cellulose Membrane ◽  
Vitro Model ◽  
Full Factorial

Clindamycin hydrochloride is a widely used antibiotic for topical use, but its main disadvantage is poor skin penetration. Therefore, new approaches in the development of clindamycin topical formulations are of great importance. We aimed to investigate the effects of the type of gelling agent (carbomer and sodium carmellose), and the type and concentration of bile acids as penetration enhancers (0.1% and 0.5% of cholic and deoxycholic acid), on clindamycin release rate and permeation in a cellulose membrane in vitro model. Eight clindamycin hydrogel formulations were prepared using a 23 full factorial design, and they were evaluated for physical appearance, pH, drug content, drug release, and permeability parameters. Although formulations with carbomer as the gelling agent exerted optimal sensory properties, carmellose sodium hydrogels had significantly higher release rates and permeation of clindamycin hydrochloride. The bile acid enhancement factors were higher in carbomer gels, and cholic acid exerted more pronounced permeation-enhancing effects. Since the differences in the permeation parameters of hydrogels containing cholic acid in different concentrations were insignificant, its addition in a lower concentration is more favorable. The hydrogel containing carmellose sodium as a gelling agent and 0.1% cholic acid as a penetration enhancer can be considered as the formulation of choice.

scholarly journals Evaluation of Skin Permeation and Analgesic Activity Effects of Carbopol Lornoxicam Topical Gels Containing Penetration Enhancer

2014 ◽  
Vol 2014 ◽  
pp. 1-9 ◽  
Author(s):  
Saleh A. Al-Suwayeh ◽  
Ehab I. Taha ◽  
Fahad M. Al-Qahtani ◽  
Mahrous O. Ahmed ◽  
Mohamed M. Badran
Keyword(s):  
Analgesic Activity ◽  
Skin Permeation ◽  
Tween 80 ◽  
Skin Penetration ◽  
Penetration Enhancers ◽  
Topical Gel ◽  
Carbopol Gel ◽  
Franz Diffusion Cells ◽  
Gel Formulations

The current study was designed to develop a topical gel formulation for improved skin penetration of lornoxicam (LOR) for enhancement of its analgesic activity. Moreover, the effect of different penetration enhancers on LOR was studied. The LOR gel formulations were prepared by using hydroxylpropyl methylcellulose (HPMC) and carbopol. The carbopol gels in presence of propylene glycol (PG) and ethanol were developed. The formulated gels were characterized for pH, viscosity, and LOR release using Franz diffusion cells. Also,in vitroskin permeation of LOR was conducted. The effect of hydroxypropylβ-cyclodextrin (HPβ-CD), beta-cyclodextrin (β-CD), Tween 80, and oleic acid on LOR permeation was evaluated. The optimized LOR gel formulation (LORF8) showed the highest flux (14.31 μg/cm2/h) with ER of 18.34 when compared to LORF3. Incorporation of PG and HPβ-CD in gel formulation (LORF8) enhanced the permeation of LOR significantly. It was observed that LORF3 and LORF8 show similar analgesic activity compared to marketed LOR injection (Xefo). This work shows that LOR can be formulated into carbopol gel in presence of PG and HPβ-CD and may be promising in enhancing permeation.

scholarly journals Effect of bile acids on electrical properties of rat colon: evaluation of an in-vitro model for secretion.

Gut ◽  
1975 ◽  
Vol 16 (6) ◽  
pp. 477-481 ◽  
Author(s):  
E J Schwiter ◽  
G W Hepner ◽  
R C Rose
Keyword(s):  
Electrical Properties ◽  
Bile Acids ◽  
In Vitro Model ◽  
Rat Colon ◽  
Vitro Model

scholarly journals Microbiological degradation of bile acids. Ring a cleavage and 7α,12α-dehydroxylation of cholic acid by Arthrobacter simplex

1969 ◽  
Vol 115 (2) ◽  
pp. 249-256 ◽  
Author(s):  
Shohei Hayakawa ◽  
Yoshiko Kanematsu ◽  
Takashi Fujiwara
Keyword(s):  
Bile Acids ◽  
Cholic Acid ◽  
Valeric Acid ◽  
Hydroxyl Groups ◽  
Partial Synthesis ◽  
Arthrobacter Simplex ◽  
Degradative Pathway ◽  
Acid Degradation

The metabolism of cholic acid by Arthrobacter simplex was investigated. This organism effected both ring a cleavage and elimination of the hydroxyl groups at C-7 and C-12 and gave a new metabolite, (4R)-4-[4α-(2-carboxyethyl)-3aα-hexahydro-7aβ-methyl-5-oxoindan-1β-yl]valeric acid, which was isolated and identified through its partial synthesis. A degradative pathway of cholic acid into this metabolite is tentatively proposed, and the possibility that the proposed pathway could be extended to the cholic acid degradation by other microorganisms besides A. simplex is discussed. The possibility that the observed reactions in vitro could occur during the metabolism of bile acids in vivo is considered.

scholarly journals The Optimization of a Dimenhydrinate Transdermal Patch Formulation Based on the Quantitative Analysis of In Vitro Release Data by DDSolver through Skin Penetration Studies

2021 ◽  
Vol 89 (3) ◽  
pp. 33
Author(s):  
Bazigha K. Abdul Rasool ◽  
Amira A. Mohammed ◽  
Yasmein Y. Salem
Keyword(s):  
Quantitative Analysis ◽  
Ex Vivo ◽  
Skin Irritation ◽  
In Vitro Release ◽  
Control Sample ◽  
Skin Penetration ◽  
Penetration Enhancers ◽  
Release Data ◽  
Skin Irritation Test

Dimenhydrinate is an over-the-counter medication that is used to relieve nausea, vomiting, and vertigo caused by motion sickness. It has a short elimination half-life, possibly due to its first-pass metabolism. The current study aimed to prepare and evaluate new transdermal formulations of dimenhydrinate to prolong the drug’s release and improve its cutaneous permeation. First, the patches were fabricated and evaluated to determine their properties. The results were statistically investigated and considered significant at the p < 0.05 level. Additionally, the quantitative analysis of the drug-release data and kinetic modeling was performed by using the DDSolver software to decide the candidate formula dependably. The effect of the penetration enhancers on the permeability of dimenhydrinate from the selected patch was then studied ex vivo compared to the control sample, and the patch’s safety was evaluated in rabbits, using the skin-irritation test.

Bile acid synthesis in isolated rat hepatocytes

1978 ◽  
Vol 56 (8) ◽  
pp. 780-783 ◽  
Author(s):  
I. M. Yousef ◽  
J. Ho ◽  
K. N. Jeejeebhoy
Keyword(s):  
Bile Acid ◽  
Bile Acids ◽  
Rat Hepatocytes ◽  
Acid Synthesis ◽  
Isolated Hepatocytes ◽  
Bile Acid Synthesis ◽  
Isolated Rat Hepatocytes ◽  
Adult Rat ◽  
Vitro Model

Normal adult rat hepatocytes were incubated for 48 h and the concentration of total and individual bile acids in homogenized samples of the culture was measured at intervals during the incubation, using radiogas chromatography and isotope derivative assay. The net increase in bile acids over the value observed at the start of the culture was taken as synthesis. The results showed that bile acid synthesis was linear up to 24 h of incubation, at a rate of 20 nmol/g hepatocytes per hour, and that 85% of the newly synthesized bile acid was cholic acid. The bile acid synthesized was mainly conjugated with taurine. These results suggest that isolated hepatocytes cultured in the way described could be a useful in vitro model for the study of bile acid synthesis.

scholarly journals Influence of bile acids on the adsorption of lidocaine and verapamil in an in vitro experiment

2010 ◽  
Vol 75 (4) ◽  
pp. 433-440 ◽  
Author(s):  
Mihalj Posa ◽  
Ksenija Kuhajda
Keyword(s):  
Hydrogen Bonds ◽  
Aqueous Medium ◽  
Bile Acids ◽  
Membrane Transport ◽  
Cholic Acid ◽  
Aqueous Phase ◽  
Vitro Experiment ◽  
In Vitro Experiment

The work is concerned with the influence of the structure of bile acids (cholic, deoxycholic, chenodeoxycholic, and their keto derivatives) on the in vitro adsorption of lidocaine and verapamil from an aqueous phase to rat's intestine membrane. Transport of lidocaine from an aqueous medium to the rat's intestine membrane was significantly increased (p < 0.05) only by 7-monoketocholic acid, whereas an analogous increase in verapamil transport was produced only by cholic acid. It appeared that, of all the tested bile acids, these two acids form the most stable complexes (by hydrogen bonds) with the respective drug.

scholarly journals Formulation of Novel Liquid Crystal (LC) Formulations with Skin-Permeation-Enhancing Abilities of Plantago lanceolata (PL) Extract and Their Assessment on HaCaT Cells

Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 1023
Author(s):  
Dóra Kósa ◽  
Ágota Pető ◽  
Ferenc Fenyvesi ◽  
Judit Váradi ◽  
Miklós Vecsernyés ◽  
...  
Keyword(s):  
Liquid Crystal ◽  
Skin Permeation ◽  
Plantago Lanceolata ◽  
Antioxidant Properties ◽  
Pharmaceutical Formulations ◽  
Biological Properties ◽  
Penetration Enhancers ◽  
Hacat Cells ◽  
Toxicity Screening

Exposure to reactive oxygen species can easily result in serious diseases, such as hyperproliferative skin disorders or skin cancer. Herbal extracts are widely used as antioxidant sources in different compositions. The importance of antioxidant therapy in inflammatory conditions has increased. Innovative formulations can be used to improve the effects of these phytopharmacons. The bioactive compounds of Plantago lanceolata (PL) possess different effects, such as anti-inflammatory, antioxidant, and bactericidal pharmacological effects. The objective of this study was to formulate novel liquid crystal (LC) compositions to protect Plantago lanceolata extract from hydrolysis and to improve its effect. Since safety is an important aspect of pharmaceutical formulations, the biological properties of applied excipients and blends were evaluated using assorted in vitro methods on HaCaT cells. According to the antecedent toxicity screening evaluation, three surfactants were selected (Gelucire 44/14, Labrasol, and Lauroglycol 90) for the formulation. The dissolution rate of PL from the PL-LC systems was evaluated using a Franz diffusion chamber apparatus. The antioxidant properties of the PL-LC systems were evaluated with 2,2-diphenyl-1-picrylhydrazyl (DPPH) and malondialdehyde (MDA) assessments. Our results suggest that these compositions use a nontraditional, rapid-permeation pathway for the delivery of drugs, as the applied penetration enhancers reversibly alter the barrier properties of the outer stratum corneum. These excipients can be safe and highly tolerable thus, they could improve the patient’s experience and promote adherence.

scholarly journals Formulation and evaluation of polyherbal anti-acne combination by using in-vitro model

2019 ◽  
Vol 10 (1) ◽  
pp. 4747-4751
Keyword(s):  
Side Effects ◽  
Drug Release ◽  
In Vitro Model ◽  
Chemical Constituents ◽  
Skin Penetration ◽  
Piper Nigrum ◽  
Synergistic Activity ◽  
Vitro Model ◽  
Global Population

Acne is one of the most common problem faced by today’s youth and is listed in eighth position in the prevalence. It is affecting almost 9.4% of the global population in the world. This skin ailment is mostly occurring in the teenagers. There is no medicine is available in the market which can cure acne. And also, there are some limitations to these available management therapies as well as side effects are associated with them. The overcome these drawbacks of the available therapies a herbal formulation can a better choice due to the easily availability, synergistic activity, better bioavailability and less side effects of phytoconstituents. For our study we have selected Raphanus sativum (Mulak), Piper nigrum (Marich) and Allium sativum (Rason) due to its uses and availability. We have estimated the chemical constituents and phytochemicals present in these plants and their activity against Propionibacterium acne. We have also prepared a formulation using all the three plants and tested them for their activity and drug release with the time. In the case of permeation study, after the 12 h study the percentage of drug release is calculated 76.65%. Finally, we are concluding that the prepared formulation and the herbs used both have the anti-acne activity and the skin penetration is good.

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