Optimization of Olive Oil-Based Nanoemulsion Preparation for Intravenous Drug Delivery

Drug Research ◽  
2018 ◽  
Vol 69 (05) ◽  
pp. 256-264 ◽  
Author(s):  
Zahra Karami ◽  
Maryam Khoshkam ◽  
Mehrdad Hamidi
Keyword(s):  
Drug Delivery ◽  
Olive Oil ◽  
Droplet Diameter ◽  
Physical Stability ◽  
Tween 80 ◽  
Intravenous Drug ◽  
Preparation Temperature ◽  
Solubility Study ◽  
In Vitro Characterization

AbstractA seven-factor Box-Behnken design was used for the optimized development of an olive oil-based nanoemulsion (NE) intended for intravenous drug delivery. The independent variables of olive oil concentration, tween 80 concentration, span 80 concentration, rate of adding of oil in aqueous phase, homogenization speed, homogenization time, and preparation temperature, were used as inputs of the factorial design. The response variables were mean droplet diameter, zeta potential (ZP), and polydispersity index (PDI). A quadratic, linear and 2FI model was established to predict the responses based on the multivariate model developed. The obtained experimental responses were in good agreement with predicted values from expert design, showing residual standard error (RSE) less than 10 %. TEM revealed that the optimized nanoemulsions were almost spherical with mean diameter about 40 nm. The developed formulation showed only about 4.6% of hemolysis and was safe for intravenous delivery. As well, the other in vitro characterization of the optimal nanoemulsion such as viscosity, percent transmittance, physical stability, and solubility study revealed it to be promising as an intravenous drug delivery system.

scholarly journals A Formulation And Characterization Of Bromocriptine Mesylate as Liquid Self nano Emulsifying Drug Delivery System

2018 ◽  
pp. 93-101 ◽  
Author(s):  
Zainab Ali Hussein
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Pituitary Tumors ◽  
Tween 80 ◽  
Drug Dissolution ◽  
Solubility Study ◽  
Ternary Phase Diagrams

Bromocriptine mesylate is a semisynthetic ergot alkaloid derivative with potent dopaminergic activity, used in the treatment of pituitary tumors, Parkinson's disease (PD), hyperprolactinaemia, neuroleptic malignant syndrome, and type 2 diabetes ,the oral bioavailability is  approximately 6%, therefore aim  its  prepare and evaluate bromocriptine mesylate  as liquid self nano emulsifying drug delivery system to enhance its solubility , dissolution and stability . Solubility study was made in different vehicles to select the best excipients for dissolving bromocriptine mesylate. Pseudo-ternary phase diagrams were constructed at 1:1, 2:1, 3:1 and 4:1 ratios of surfactant and co-surfactant, four formulations were prepared using various concentrations of castor oil, tween 80 and ethanol. All prepared formulations were evaluated for particle size distribution, polydispersity index, drug content, thermodynamic stability, dispersibility and emulsification time, robustness to dilution and in vitro drug dissolution. It was found that release rate and extent for all prepared formulations were significantly higher (p < 0.05) than plain drug powder. from the study, it was concluded that self-nanoemulsifying drug delivery system is a promising approach to improve solubility, dissolution, and stability of bromocriptine mesylate.

Novel Self-Micro Emulsifying Drug Delivery System for safe intra muscular delivery with improved pharmacodynamics and pharmacokinetics

2021 ◽  
Vol 18 ◽  
Author(s):  
Subheet Kumar Jain ◽  
Neha Panchal ◽  
Amrinder Singh ◽  
Shubham Thakur ◽  
Navid Reza Shahtaghi ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Inflammatory Diseases ◽  
Diclofenac Sodium ◽  
Physical Stability ◽  
In Vivo Studies ◽  
High Concentration

Background: Diclofenac sodium (DS) injection is widely used in the management of acute or chronic pain and inflammatory diseases. It incorporates 20 % w/v Transcutol-P as a solubilizer to make the stable injectable formulation. However, the use of Transcutol-P in high concentration leads to adverse effects such as severe nephrotoxicity, etc. Some advancements resulted in the formulation of an aqueous based injectable but that too used benzyl alcohol reported to be toxic for human use. Objective: To develop an injectable self-micro emulsifying drug delivery system (SMEDDS) as a novel carrier of DS for prompt release with better safety and efficacy. Methods: A solubility study was performed with different surfactants and co-surfactants. The conventional stirring method was employed for the formulation of SMEDDS. Detailed in vitro characterization was done for different quality control parameters. In vivo studies were performed using Wistar rats for pharmacokinetic evaluation, toxicological analysis, and analgesic activity. Results: The optimized formulation exhibited good physical stability, ideal globule size (156±0.4 nm), quick release, better therapeutics, and safety, increase in LD50 (221.9 mg/kg) to that of the commercial counterpart (109.9 mg/kg). Further, pre-treatment with optimized formulation reduced the carrageenan-induced rat paw oedema by 88±1.2 % after 4 h, compared to 77±1.6 % inhibition with commercial DS formulation. Moreover, optimized formulation significantly (p<0.05) inhibited the pain sensation in the acetic-acid induced writhing test in mice compared to its commercial equivalent with a better pharmacokinetic profile. Conclusion: The above findings confirmed that liquid SMEDDS could be a successful carrier for the safe and effective delivery of DS

scholarly journals Formulation, characterization, evaluation and in vitro study of transfersomal gel medroxyprogesterone acetate for transdermal drug delivery

2020 ◽  
Vol 11 (4) ◽  
pp. 5373-5381
Author(s):  
Iskandarsyah ◽  
Camelia Dwi Putri Masrijal ◽  
Harmita
Keyword(s):  
Drug Delivery ◽  
Medroxyprogesterone Acetate ◽  
Transdermal Drug Delivery ◽  
High Performance ◽  
Hormonal Contraception ◽  
In Vitro Study ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Reversed Phase

A hormonal contraception progestin such as medroxyprogesterone acetate (MPA) is used to helps regulate ovulation thus as a part of contraception hormone therapy as a method of birth control. This study aimed to formulate, characterized, evaluated transfersomal gel containing medroxyprogesterone acetate and to increased subcutaneous penetration of medroxyprogesterone acetate. In this research, three transfersomes formulas were prepared and optimized, e.g. F1, F2 and F3 with phosphatidylcholine: tween 80 concentration were 90:10; 85:15; and 75:25, respectively. F2 was the best formula with the highest entrapment efficiency 81.20±0.42 %, Average 81.35 ±0.78 nm, morphology of vesicles were spheres, indeks polidispersity 0.198±0.012 and zeta potential was -34.83±0.64 mV. The transpersonal gel (FGT) containing F2, and non-transpersonal gel containing MPA in methanol(FG) were prepared. In vitro penetration test were conducted to both of them using Franz Diffusion cells. Analysis of medroxyprogesterone acetate used a high performance liquid chromatographic (HPLC) method with an ultraviolet detector on reversed-phase C18, 5µm; 150 x 4.6 mmcolumn; using acetonitrile-0.1% formic acid (60:40/v:v) and was detected at a wavelength of 240 nm with flow rate at 1.0 mL/min. Gel stability evaluation results showed that FGT was better than FG on pH stability, viscosity and rheological properties. Based on in vitro penetration study, cumulative subcutaneous penetration of medroxyprogesterone acetate from FGT was 2356.45 ± 197.73 ng.cm-2 and from FG 359.15 ± 13.60 ng.cm-2, respectively. Flux value for FGT and FG were 112.77 ± 6,47 ng.cm-2.hr-1and 17.99 ± 4.81 ng.cm-2.hr-1, respectively. It could be concluded that transfersomal gel medroxyprogesterone acetate for transdermal drug delivery increased cumulative transdermal penetration of medroxyprogesterone acetate by six times more than non-transfersomal gel dosage form.

SELF-EMULSIFYING DRUG DELIVERY SYSTEM CONTAINING ACECLOFENAC: DESIGN & DEVELOPMENT USING QUALITY BY DESIGN (QBD) CONCEPT

INDIAN DRUGS ◽  
2014 ◽  
Vol 51 (06) ◽  
pp. 16-26
Author(s):  
V Suthar ◽  
◽  
M Gokel ◽  
S Butani ◽  
A Solanki
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Dosage Form ◽  
Quality By Design ◽  
Tween 80 ◽  
Current Approach ◽  
In Vitro Dissolution ◽  
Design Development

The aim of the present study was to develop self-emulsifying drug delivery system (SEDDS) of aceclofenac for potential improvement in the in vitro dissolution. The Food and Drug Control Agency (FDCA) has put more stress on the quality, safety and efficacy of the dosage form. The use of design of experiments and quality by Design (QbD) in the development of self emulsifying drug delivery system (SEDDS) containing aceclofenac is demonstrated. The optimum formulation contained Labrafil M 1944 CS, Tween 80 and Transcutol P. The systematic approach enabled us in identifying the design space. The results revealed that while devising the control strategies during manufacturing, more attention should be focused on the ratios of oil to surfactant and surfactant to co-surfactant. The drug was released at a faster rate due to a large surface area. The current approach enabled us to develop a dosage form which is economic, patient-friendly and does not require assistance of a doctor or nurse, especially at remote places at odd hours.

scholarly journals Investigation Utilizing the HLB Concept for the Development of Moisturizing Cream and Lotion: In-Vitro Characterization and Stability Evaluation

Cosmetics ◽  
2020 ◽  
Vol 7 (2) ◽  
pp. 43 ◽  
Author(s):  
Shoaib Alam ◽  
Mohammed S. Algahtani ◽  
Mohammad Zaki Ahmad ◽  
Javed Ahmad
Keyword(s):  
Physical Stability ◽  
Storage Conditions ◽  
Phase System ◽  
Stability Evaluation ◽  
Stable Emulsion ◽  
Promising Strategy ◽  
In Vitro Characterization ◽  
Hydrophilic Lipophilic Balance ◽  
Droplet Morphology

The current study aims to utilize the concept of the hydrophilic–lipophilic balance (HLB) value of ingredients for the development of a stable emulsion-based moisturizing cream and lotion for cosmetic application. The combination of a hydrophilic and lipophilic emulsifier such as glyceryl stearate (HLB value 3.8) and PEG-100 stearate (HLB value 18.8) were found to be effective to emulsify the chosen oil phase system at a specific concentration to achieve the required HLB for the development of the stable emulsion-based system. The developed formulation was characterized for pH, viscosity, spreadability, rheology, and droplet morphology. The influence of carbopol® ETD 2020 and the concentration of the oil phase on the rheology of the product was investigated and found to be significant to achieve the required thickening to convert the lotion into a cream. The formulation system developed through utilizing the concept of HLB was compared to a product developed through the conventional approach. It was observed that the utilization of the HLB method for the development of an emulsion-based product is a promising strategy compared to the conventional method. The physical stability and thermodynamic stability tests were carried out under different storage conditions. It was observed that the developed formulation was able to retain its integrity without showing any signs of instability during storage.

scholarly journals Porous Bioactive Glass Scaffolds for Local Drug Delivery in Osteomyelitis: Development and In Vitro Characterization

2010 ◽  
Vol 11 (4) ◽  
pp. 1675-1683 ◽  
Author(s):  
Chidambaram Soundrapandian ◽  
Someswar Datta ◽  
Biswanath Kundu ◽  
Debabrata Basu ◽  
Biswanath Sa
Keyword(s):  
Drug Delivery ◽  
Bioactive Glass ◽  
Local Drug Delivery ◽  
In Vitro Characterization
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