scholarly journals Development of ionic liquid microemulsion for transdermal delivery of a chemotherapeutic agent

2021 ◽  
Vol 3 (2) ◽  
Author(s):  
Harish Sharma ◽  
Gyanesh Kumar Sahu ◽  
Chanchal Deep Kaur
Keyword(s):  
Skin Cancer ◽  
Drug Release ◽  
Drug Carrier ◽  
Tween 80 ◽  
Cost Effective ◽  
Topical Administration ◽  
Skin Permeability ◽  
Continuous Exposure ◽  
Topical Gel ◽  
Area Of Concern

AbstractNowadays skin cancers have become a major area of concern because of the continuous exposure to sun rays (UV rays). Hence, the present work focused on the synthesis of an innovative 5-Fluorouracil (5-FU) microemulsion as a topical delivery system mainly used to treat various forms of skin cancer. The topical administration of most of the active compounds is impaired by limited skin permeability due to the presence of skin barriers. In this sequence, the microemulsion represents a cost-effective and convenient drug carrier system that successfully delivers the drug to and across the skin. Unfortunately, 5-FU reveals high toxicity and low tumor affinity became inefficient for patients with the risk of serious side effects. For decreasing of eluding some of its disadvantages we made it more effective by preparing its microemulsion with tween 80 (surfactant), isopropyl alcohol (co-surfactant), oleic acid (oil) in a four-component system. This study emphasized increasing the drug release by multiple times and a topical gel has been formulated and designs to elongate the drug release. All preparation of 5-FU microemulsion was characterized by physicochemical and drug release studies. The size of the 5-FU microemulsion was 550–600 nm confirmed by transmission electron microscopy (TEM) and Zetasizer. The clear microemulsion was prepared at pH 5–6. It shows viscosity in the limit of 13.52–18.23 Pa s. The outcome of the present work is satisfactory for skin cancer treatment.

Formulation, Design and Development of Niosome Based Topical Gel for Skin Cancer

2017 ◽  
Vol 2 (3) ◽  
Keyword(s):  
Skin Cancer ◽  
Drug Release ◽  
Hemorrhagic Cystitis ◽  
The Body ◽  
Cancer Drug ◽  
Inversion Method ◽  
Body Parts ◽  
Basal Cells ◽  
Formulation Design ◽  
Topical Gel

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.

scholarly journals FORMULATION AND EVALUATION OF CEFIXIME TRIHYDRATE TOPICAL GEL FOR WOUND INFECTIONS

2018 ◽  
Vol 11 (8) ◽  
pp. 369
Author(s):  
Uma Shankar Marakanam Srinivasan ◽  
Vishnu Vishnu ◽  
Sharmila Sharmila ◽  
Amod Kumar
Keyword(s):  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Research Work ◽  
Topical Administration ◽  
Generation Cephalosporin ◽  
Wound Infections ◽  
Topical Gel ◽  
Carbopol 940 ◽  
Gel Formulations

Objective: The objective of this research work was to formulate and evaluate topical gel loaded with cefixime trihydrate, a third-generation cephalosporin antibiotic for the treatment of bacterial wound infections.Methods: The cefixime trihydrate gel was formulated using polymers such as Carbopol 940 and hydroxypropyl methylcellulose E4M in varying concentrations. Three different formulations were prepared and characterized physically for color, syneresis, spreadability, pH, drug content, and rheological properties. In vitro drug release in phosphate buffer pH 7.4 and antibacterial study were performed for the gel formulation to evaluate its therapeutic effect on wound infections.Results: The study demonstrated that the gel formulations showed promising results on their physical evaluation tests. The rheology behavior of the gel was shear-thinning flow type which indicated easy spreading of the gel. The drug release of the gel formulation F2 was selected as the best due to its highest drug release rate of 32.2% in comparison with the other two formulations after 2 h of the study. F2 formulation possessed the highest antibacterial activity as compared to other two formulations.Conclusion: A pioneering work was done on formulating cefixime trihydrate as a gel for topical administration. The antibacterial effect of the drug as gel formulation showed promising effect. We conclude that the cefixime trihydrate could be successively loaded into a gel formulation and can be used for effectively for wound infections like diabetic foot wounds.

scholarly journals Development and Invitro Evaluation of Solid Lipid Nano Particles Loaded Topical Gel Containing Combination of Drugs Used In The Better Therapy of Psoriasis

2021 ◽  
Vol 11 (6) ◽  
pp. 21-33
Author(s):  
Suryakumari Chalakanti ◽  
Narender Malothu
Keyword(s):  
Drug Release ◽  
Drug Loading ◽  
Topical Therapy ◽  
Research Work ◽  
Tween 80 ◽  
Homogenization Method ◽  
Nano Particles ◽  
Loading Capacity ◽  
Topical Gel ◽  
Solid Lipid

The present research work was aimed to develop a Solid lipid nanoparticles (SLNs) based topical gel for the treatment of psoriasis. SLNs were prepared and then incorporated in a topical gel as a carrier. High-Pressure Homogenization method was used to improved drug loading capacity and drug release properties. Excipients like Compritol 888 ATO, Tween 80,Precirol ATO5, Poloxamer407, Cremophor RH40, Carpobol 934, Methyl Paraben, TEA, Distilled water were used. The optimized formulations were based on Zeta potential, analysis of particle size, differential scanning Colorimetery, scanning electron microscopy and study of Invitro drug release. The present research study revealed that the SLNs based Gel containing F4 formulation could potentially exploit as a carrier with improved drug loading capacity and drug release properties. Thus, tacrolimus loaded SLNs formulation can be beneficial in the treatment of psoriasis. It was concluded that the prepared formulation can be used for treatment of psoriasis by using the topical therapy of nanogel and this will attempt to increase the efficacy of the drug at the site of action.

Development and Optimization of Sustained Release Moxifloxacin Hydrochloride Loaded Nanoemulsion for Ophthalmic Drug Delivery: A 32 Factorial Design Approach

2020 ◽  
Vol 12 ◽  
Author(s):  
Sagar R. Pardeshi ◽  
Harshal A. Mistari ◽  
Rakhi S. Jain ◽  
Pankaj R. Pardeshi ◽  
Rahul L. Rajput ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Factorial Design ◽  
Water Solubility ◽  
Tween 80 ◽  
Drug Release Profile ◽  
Sustained Drug Release ◽  
Bacterial Conjunctivitis ◽  
Promising Alternative

Background: Moxifloxacin is a BCS class I drug used in the treatment of bacterial conjunctivitis and keratitis. Despite its high water solubility, it possesses limited bioavailability due to anatomical and physiological constraints associated with the eyes which required multiple administrations to achieve a therapeutic effect. Objective: In order to prolong drug release and to improve antibacterial efficacy for the treatment of bacterial keratitis and conjunctivitis, moxifloxacin loaded nanoemulsion was developed. Methods: The concentration of oil (oleic acid), surfactant (tween 80), and cosurfactant (propylene glycol) were optimized by employing a 3-level 2-factorial design of experiment for the development of nanoemulsion. The developed nanoemulsion was characterized by particle size distribution, viscosity, refractive index, pH, drug content and release, transmission electron microscopy (TEM), and antibacterial study. The compatibility of the drug with the excipients was accessed by Fourier transform infrared spectroscopy (FTIR). Result: The average globule size was found to be 198.20 nm. The TEM study reveals the globules were nearly spherical and are well distributed. In vitro drug release profile for nanoemulsion shown sustained drug release (60.12% at the end of 6 h) compared to drug solution, where complete drug released within 2 h. The antibacterial effectiveness of the drug-loaded nanoemulsion was improved against S. aureus compared with the marketed formulation. Conclusion: The formulated sustained release nanoemulsion could be a promising alternative to eye drop with improved patient compliance by minimizing dosing frequency with improved antibacterial activity.

scholarly journals Non-invasive skin sampling of tryptophan/kynurenine ratio in vitro towards a skin cancer biomarker

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Skaidre Jankovskaja ◽  
Johan Engblom ◽  
Melinda Rezeli ◽  
György Marko-Varga ◽  
Tautgirdas Ruzgas ◽  
...  
Keyword(s):  
Skin Cancer ◽  
Relative Increase ◽  
Cancer Biomarker ◽  
Cancer Diagnostics ◽  
Sampling Time ◽  
Skin Permeability ◽  
Experimental Conditions ◽  
Non Invasive

AbstractThe tryptophan to kynurenine ratio (Trp/Kyn) has been proposed as a cancer biomarker. Non-invasive topical sampling of Trp/Kyn can therefore serve as a promising concept for skin cancer diagnostics. By performing in vitro pig skin permeability studies, we conclude that non-invasive topical sampling of Trp and Kyn is feasible. We explore the influence of different experimental conditions, which are relevant for the clinical in vivo setting, such as pH variations, sampling time, and microbial degradation of Trp and Kyn. The permeabilities of Trp and Kyn are overall similar. However, the permeated Trp/Kyn ratio is generally higher than unity due to endogenous Trp, which should be taken into account to obtain a non-biased Trp/Kyn ratio accurately reflecting systemic concentrations. Additionally, prolonged sampling time is associated with bacterial Trp and Kyn degradation and should be considered in a clinical setting. Finally, the experimental results are supported by the four permeation pathways model, predicting that the hydrophilic Trp and Kyn molecules mainly permeate through lipid defects (i.e., the porous pathway). However, the hydrophobic indole ring of Trp is suggested to result in a small but noticeable relative increase of Trp diffusion via pathways across the SC lipid lamellae, while the shunt pathway is proposed to slightly favor permeation of Kyn relative to Trp.

scholarly journals 3D Printed Microfluidic Devices for Drug Release Assays

Pharmaceutics ◽  
2020 ◽  
Vol 13 (1) ◽  
pp. 13
Author(s):  
Benzion Amoyav ◽  
Yoel Goldstein ◽  
Eliana Steinberg ◽  
Ofra Benny
Keyword(s):  
3D Printing ◽  
Drug Release ◽  
Particle Production ◽  
Cost Effective ◽  
Drug Dissolution ◽  
Cytotoxicity Test ◽  
High Durability ◽  
One Step ◽  
Cost Effective Alternative ◽  
Multiple Recycling

Microfluidics research for various applications, including drug delivery, cell-based assays and biomedical research has grown exponentially. Despite this technology’s enormous potential, drawbacks include the need for multistep fabrication, typically with lithography. We present a one-step fabrication process of a microfluidic chip for drug dissolution assays based on a 3D printing technology. Doxorubicin porous and non-porous microspheres, with a mean diameter of 250µm, were fabricated using a conventional “batch” or microfluidic method, based on an optimized solid-in-oil-in-water protocol. Microspheres fabricated with microfluidics system exhibited higher encapsulation efficiency and drug content as compared with batch formulations. We determined drug release profiles of microspheres in varying pH conditions using two distinct dissolution devices that differed in their mechanical barrier structures. The release profile of the “V” shape barrier was similar to that of the dialysis sac test and differed from the “basket” barrier design. Importantly, a cytotoxicity test confirmed biocompatibility of the printed resin. Finally, the chip exhibited high durability and stability, enabling multiple recycling sessions. We show how the combination of microfluidics and 3D printing can reduce costs and time, providing an efficient platform for particle production while offering a feasible cost-effective alternative to clean-room facility polydimethylsiloxane-based chip microfabrication.

Development and Validation of UV-Visible Spectrophotometric method for the Estimation of Curcumin and Tetrahydrocurcumin in Simulated Intestinal Fluid

2021 ◽  
pp. 2971-2975
Author(s):  
Jai Bharti Sharma ◽  
Sherry Sherry ◽  
Shailendra Bhatt ◽  
Vipin Saini ◽  
Manish Kumar
Keyword(s):  
Drug Release ◽  
Spectrophotometric Method ◽  
Tween 80 ◽  
Solvent System ◽  
Intestinal Fluid ◽  
Simulated Intestinal Fluid ◽  
Validation Parameters ◽  
Administration Method ◽  
Uv Visible ◽  
Development And Validation

Background: Due to solubility issues of curcumin and tetrahydrocurcumin, there is a need for the development of a UV-Visible spectrophotometric method that can estimate the drug release precisely and accurately. The addition of surfactant in the dissolution medium in low concentration achieved bio-comparable surface activity and can be used to estimate the drug release from formulations by avoiding sink conditions. Objective: The purpose of the present investigation was to develop a simple and précise UV-Visible spectrophotometric method for the determination of curcumin and tetrahydrocurcumin after oral administration. Method: A UV-Visible spectrophotometric method was developed using an appropriate solvent system for the estimation of curcumin and tetrahydrocurcumin. The solvent system having simulated intestinal fluid and particular concentration of surfactant was selected and further validated according to guidelines of the international conference on harmonization (ICH), the analytical parameter like linearity, precision and accuracy, etc. were studied. Results: Simulated intestinal fluid pH 7.4 with tween 80 at 1 % concentration satisfied all the conditions relative to peak quality at the stated wavelength for curcumin and intestinal fluid pH 7.4 with tween 80 at 0.5% concentration satisfied all the conditions relative to Peak quality at the stated wavelength for tetrahydrocurcumin. The developed methods were found within the range of all the validation parameters. Conclusion: The proposed method was found to be very simple and precise and can be used for routine quantitative analysis of curcumin and tetrahydrocurcumin.

scholarly journals Effect of nonionic surfactants on the release of paracetamol from suppositories

2015 ◽  
Vol 26 (1) ◽  
pp. 40-44
Keyword(s):  
Drug Release ◽  
Physical Properties ◽  
Phosphate Buffer ◽  
Nonionic Surfactants ◽  
Tween 80 ◽  
Content Uniformity ◽  
Fusion Method ◽  
Disintegration Time ◽  
Span 60

The preparation suppositories contain 250 mg of paracetamol on different bases using Novata BD, Novata BCF and composition of Novata BCF/BD (1:1). Suppositories were prepared by the fusion method. The prepared formulations with or without surfactants (Tween 80, Span 60) at concentrations of 2% and 4% (w/w) were tested for hardness, to tal time of de for ma tion, disintegration time, content uniformity and release of the drug. The release of the drug was carried in the apparatus with the stirrer shade in phosphate buffer (pH 7.2) at 100 rpm. The physical properties of the prepared suppositories were according with the requirement of Polish Pharmacopoeia 9th edition. Addition of 4 % Tween 80 to suppository bases significantly increased the drug release from all the investigated formulations. However, incorporation of Span 60 did not result in improvement of the drug release significantly.

scholarly journals Formulation, Development and Evaluation of Ibuprofen Loaded Nano-transferosomal Gel for the Treatment of Psoriasis

2019 ◽  
pp. 1-8
Author(s):  
Marwa H. Abdallah ◽  
Amr S. Abu Lila ◽  
Md. Khalid Anwer ◽  
El-Sayed Khafagy ◽  
Muqtader Mohammad ◽  
...  
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Formulation Development ◽  
In Vitro Drug Release ◽  
Vesicle Size

The present work was aimed to develop a transferosomal gel of ibuprofen (IBU) for the amelioration of psoriasis like inflammation. Three formulation of IBU loaded transferosomes (TFs1-TFs3) were prepared using different proportions of lipid (phospholipon 90H) and surfactant (tween 80) and further evaluated for vesicle size, zeta potential (ZP), entrapment efficiency and in vitro drug release. The IBU loaded transferosomes (TFs2) was optimized with vesicle size (217±8.4 nm), PDI (0.102), ZP (-31.5±4.3 mV), entrapment efficiency (88.4±6.9%) and drug loading (44.2±2.9%). Further, the optimized IBU loaded transferosomes (TFs2) was incorporated into 1% carbopol 934 gel base and characterized for homogeneity, extrudability, viscosity and drug content. The in vivo pharmacodynamic study of gel exhibited reduction in psoriasis like inflammation in mice. The ibuprofen loaded transferosomal gel was successfully developed and has shown the potential to be a new therapy against psoriasis like inflammation.

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