Pro-drugs as drug delivery systems XI. Preparation and characterization of a novel water-soluble pro-drug type for barbituric acids

1980 ◽  
Vol 6 (1) ◽  
pp. 19-27 ◽  
Author(s):  
Hans Bundgaard ◽  
Erik Falch ◽  
Claus Larsen
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Delivery Systems ◽  
Water Soluble ◽  
Drug Type

Development of lipid nanocarriers for tuberculosis treatment: evaluation of suitable excipients and nanocarriers

2021 ◽  
Vol 18 ◽  
Author(s):  
Gabriela Hädrich ◽  
Cristiana Lima Dora ◽  
Gustavo Richter Vaz ◽  
Raphael Boschero ◽  
Arthur Sperry Appel ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Physicochemical Characterization ◽  
Entrapment Efficiency ◽  
Delivery Systems ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
Lipid Nanocarriers ◽  
Low Toxicity

Background: Lipid nanocarriers have been widely tested as drug delivery systems to treat diseases due to their bioavailability, controlled release, and low toxicity. For the pulmonary route, the Food and Drug Administration favors the use of substances generally recognized as safe, as well as biodegradable and biocompatible to minimize the possibility of toxicity. Tuberculosis (TB) remains a public health threat worldwide, mainly due to the long treatment duration and adverse effects. Therefore, new drug delivery systems to treat TB are needed. Objective: Physicochemical characterization of different lipid-based nanocarriers was used to optimize carrier properties. Optimized systems were incubated with Mycobacterium tuberculosis to assess whether lipid-based systems act as an energy source for the bacteria, which could be counterproductive to therapy. Method: Several excipients and surfactants were evaluated to prepare different types of nanocarriers using high-pressure homogenization. Results: A mixture of trimyristin with castor oil was chosen as the lipid matrix after differential scanning calorimetry analysis. A mixture of egg lecithin and PEG-660 stearate was selected as an optimal surfactant system as this mixture formed the most stable formulations. Three types of lipid nanocarriers, solid lipid nanoparticles, nanostructured lipid carriers (NLC), and Nano emulsions, were prepared, with the NLC systems showing the most suitable properties for further evaluation. It may provide the advantages of increasing the entrapment efficiency, drug release, and the ability to be lyophilized, producing powder for pulmonary administration being an alternative to entrap poor water-soluble molecules. Conclusion: Furthermore, the NLC system can be considered for use as a platform for the treatment of TB by the pulmonary route.

Biopolymers with Medical Applications Optimized method for obtaining chitosan-based delivery systems

2018 ◽  
Vol 69 (7) ◽  
pp. 1756-1759 ◽  
Author(s):  
Luminita Confederat ◽  
Iuliana Motrescu ◽  
Sandra Constantin ◽  
Florentina Lupascu ◽  
Lenuta Profire
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Average Diameter ◽  
Delivery Systems ◽  
Cross Linking ◽  
Low Molecular Weight ◽  
Polymeric Systems ◽  
Chitosan Microparticles ◽  
Degree Of Swelling

The aim of this study was to optimize the method used for obtaining microparticles based on chitosan � a biocompatible, biodegradable, and nontoxic polymer, and to characterize the developed systems. Chitosan microparticles, as drug delivery systems were obtained by inotropic gelation method using pentasodiumtripolyphosphate (TPP) as cross-linking agent. Chitosan with low molecular weight (CSLMW) in concentration which ranged between 0.5 and 5 %, was used while the concentration of cross-linking agent ranged between 1 and 5%. The characterization of the microparticles in terms of shape, uniformity and adhesion was performed in solution and dried state. The size of the microparticles and the degree of swelling were also determined. The structure and the morphology of the developed polymeric systems were analyzed by Fourier transform infrared spectroscopy (FTIR) and scanning electron microscopy (SEM).The average diameter of the chitosan microparticles was around 522 �m. The most stable microparticles were obtained using CSLMW 1% and TPP 2% or CSLMW 0.75%and TPP 1%. The micropaticles were spherical, uniform and without flattening. Using CSLMW in concentration of 0.5 % poorly cross-linked and crushed microparticles have been obtained at all TPP concentrations. By optimization of the method, stable chitosan-based micropaticles were obtained which will be used to develop controlled release systems for drug delivery.

scholarly journals Low molecular mass chitosan as carrier for a hydrodynamically balanced system for sustained delivery of ciprofloxacin hydrochloride

2012 ◽  
Vol 62 (2) ◽  
pp. 237-250 ◽  
Author(s):  
Anurag Verma ◽  
Ashok Bansal ◽  
Amitava Ghosh ◽  
Jayanta Pandit
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Molecular Mass ◽  
Drug Delivery Systems ◽  
Delivery Systems ◽  
Water Soluble ◽  
Sustained Delivery ◽  
Ciprofloxacin Hydrochloride ◽  
Water Soluble Drug ◽  
Major Interest

Low molecular mass chitosan as carrier for a hydrodynamically balanced system for sustained delivery of ciprofloxacin hydrochloride Chitosan has become a focus of major interest in recent years due to its excellent biocompatibility, biodegradability and non-toxicity. Although this material has already been extensively investigated in the design of different types of drug delivery systems, it is still little explored for stomach specific drug delivery systems. The objective of the present investigation was to explore the potential of low molecular mass chitosan (LMCH) as carrier for a hydrodynamically balanced system (HBS) for sustained delivery of water soluble drug ciprofloxacin hydrochloride (CP). Various formulations were prepared by physical blending of drug and polymer(s) in varying ratios followed by encapsulation into hard gelatin capsules. All the formulations remained buoyant in 0.1 mol L-1 HCl (pH 1.2) throughout the experiment. Effect of addition of xanthan gum (XG) or ethyl cellulose (EC) on drug release was also investigated. Zero order drug release was obtained from the formulations containing LMCH alone or in combination with XG, and in one instance also with EC. Our results suggest that LMCH alone or in combination with XG is an excellent material for stomach specific sustained delivery of CP from hydrodynamically balanced single unit capsules.

Innovative Strategies for Lipid-Based Drug Delivery

2018 ◽  
pp. 60-84 ◽  
Author(s):  
Navneet Sharma ◽  
Sabna Kotta ◽  
Mohd Aleem ◽  
Shubham Singh ◽  
Rakesh Kumar Sharma
Keyword(s):  
Drug Delivery ◽  
Drug Absorption ◽  
Drug Delivery Systems ◽  
Delivery Systems ◽  
Water Soluble ◽  
Absorption Process ◽  
Innovative Strategies ◽  
The Poor ◽  
Water Soluble Drugs ◽  
Selection Of

In the last decade, there has been a mounting concern in lipid-based formulations to deliver water-soluble drugs. Lipid-based drug delivery systems are one of the budding and promising technologies designed to tackle the poor bioavailability problems. This chapter stresses the different mechanisms of lipophilic drug absorption along with its advantages and limitations. It points out the different mechanisms of how lipid-based excipients and the different formulations interact with the absorption process. This review provides a comprehensive summary about the lipid formulation classification scheme (LFCS), a guide for the selection of appropriate formulation and commonly used excipients for lipid-based formulations, along with the important factors to be considered in formulation design and excipient selection. This review also focuses on the formulation of solid lipid-based formulations, important evaluation aspects, and commercial formulations available for the purpose.

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