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.

Analytical Approaches to the Characterization of Solid Drug Delivery Systems with Porous Adsorbent Carriers

2018 ◽  
Vol 25 (33) ◽  
pp. 3956-3972
Author(s):  
Marko Krstić ◽  
Slavica Ražić
Keyword(s):  
Drug Delivery ◽  
Infrared Spectroscopy ◽  
Drug Delivery Systems ◽  
Analytical Techniques ◽  
Delivery Systems ◽  
Scanning Calorimetry ◽  
Advantages And Disadvantages ◽  
Target Drug ◽  
Analytical Approaches

A large variety of analytical techniques are available to meet the needs of characterization of solid samples. But, when solid drug delivery systems are concerned we are faced with demanding methodologies which have to compile capabilities of analytical techniques in regard to large diversity of structures and surface functionality of analyzed adsorbent carriers. In this review, the most commonly used analytical techniques are presented with their basic principles, advantages and disadvantages in applications of interest. Adsorbent carriers are widely used today as ingredients in the formulation of pharmaceutical forms, for increasing the dissolution rate of the drug and hence the bioavailability. They are also used in the formulation of substances with modified or target drug release into a specific tissue. Methods of thermal analysis (Thermogravimetry - TGA, Differential Scanning Calorimetry - DSC and Thermal microscopy - TM), spectroscopic methods (Infrared Spectroscopy - IR, especially Fourier Transform Infrared Spectroscopy - FTIR and Raman spectroscopy), crystallographic methods (Powder X-Ray Diffraction - PXRD) and finally Scanning Electron Microscopy (SEM) are the most powerful in the characterization of modern therapeutic systems with porous adsorbents. The problem-solving power of each particular analytical method is often enhanced by using simultaneous methods rather than a single technique.

scholarly journals Physicochemical Characterization of Hyaluronic Acid and Chitosan Liposome Coatings

2021 ◽  
Vol 11 (24) ◽  
pp. 12071
Author(s):  
Claudia Bonechi ◽  
Gabriella Tamasi ◽  
Alessandro Donati ◽  
Gemma Leone ◽  
Marco Consumi ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Hyaluronic Acid ◽  
Drug Delivery Systems ◽  
Secondary Ion Mass Spectrometry ◽  
Synergistic Effects ◽  
Physicochemical Characterization ◽  
Chemical Properties ◽  
Delivery Systems ◽  
Specific Chemical

Hyaluronic acid (HA) and chitosan (CH) are biopolymers that are widely used in many biomedical applications and for cosmetic purposes. Their chemical properties are fundamental to them working as drug delivery systems and improving their synergistic effects. In this work, two different protocols were used to obtain zwitterionic liposomes coated with either hyaluronic acid or chitosan. Specifically, the methodologies used to perform vesicle preparation were chosen by taking into account the specific chemical properties of these two polysaccharides. In the case of chitosan, liposomes were first synthesized and then coated, whereas the coating of hyaluronic acid was achieved through lipidic film hydration in an HA aqueous solution. The size and the zeta-potential of the polysaccharide-coated liposomes were determined by dynamic light scattering (DLS). This approach allowed coated liposomes to be obtained with hydrodynamic diameters of 264.4 ± 12.5 and 450.3 ± 16.7 nm for HA- and CH-coated liposomes, respectively. The chemical characterization of the coated liposomal systems was obtained by surface infrared (ATR-FTIR) and nuclear magnetic resonance (NMR) spectroscopies. In particular, the presence of polysaccharides was confirmed by the bands assigned to amides and saccharides being in the 1500–1700 cm−1 and 800–1100 cm−1 regions, respectively. This approach allowed confirmation of the efficiency of the coating processes, evidencing the presence of HA or CH at the liposomal surface. These data were also supported by time-of-flight secondary ion mass spectrometry (ToF-SIMS), which provided specific assessments of surface (3–5 nm deep) composition and structure of the polysaccharide-coated liposomes. In this work, the synthesis and the physical chemistry characterization of coated liposomes with HA or CH represent an important step in improving the pharmacological properties of drug delivery systems.

scholarly journals Soluplus Graft Copolymer: Potential Novel Carrier Polymer in Electrospinning of Nanofibrous Drug Delivery Systems for Wound Therapy

2014 ◽  
Vol 2014 ◽  
pp. 1-7 ◽  
Author(s):  
Urve Paaver ◽  
Ingrid Tamm ◽  
Ivo Laidmäe ◽  
Andres Lust ◽  
Kalle Kirsimäe ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Wound Healing ◽  
Graft Copolymer ◽  
Drug Delivery Systems ◽  
Amorphous State ◽  
Delivery Systems ◽  
Water Soluble ◽  
Synthetic Graft ◽  
Scanning Calorimetry ◽  
Poorly Water Soluble

Electrospinning is an effective method in preparing polymeric nanofibrous drug delivery systems (DDSs) for topical wound healing and skin burn therapy applications. The aim of the present study was to investigate a new synthetic graft copolymer (Soluplus) as a hydrophilic carrier polymer in electrospinning of nanofibrous DDSs. Soluplus (polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (PCL-PVAc-PEG)) was applied in the nonwoven nanomats loaded with piroxicam (PRX) as a poorly water-soluble drug. Raman spectroscopy, X-ray powder diffraction, differential scanning calorimetry, and scanning electron microscopy (SEM) were used in the physical characterization of nanofibrous DDSs. According to the SEM results, the drug-loaded PCL-PVAc-PEG nanofibers were circular in cross-section with an average diameter ranging from 500 nm up to 2 µm. Electrospinning stabilized the amorphous state of PRX. In addition, consistent and sustained-release profile was achieved with the present nanofibrous DDSs at the physiologically relevant temperature and pH applicable in wound healing therapy. In conclusion, electrospinning can be used to prepare nanofibrous DDSs of PCL-PVAc-PEG graft copolymer (Soluplus) and to stabilize the amorphous state of a poorly water-soluble PRX. The use of this synthetic graft copolymer can open new options to formulate nanofibrous DDSs for wound healing.

scholarly journals Development of Lipid-Based Drug Delivery Systems for Gene Therapy: Physicochemical Characterization of Charged Lipid Interactions

2016 ◽  
Vol 110 (3) ◽  
pp. 247a
Author(s):  
Bashe Y. Bashe ◽  
Sherry S.W. Leung ◽  
Karelia H. Delgado-Magnero ◽  
Mohsen Ramezanpour ◽  
Pieter R. Cullis ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Gene Therapy ◽  
Drug Delivery Systems ◽  
Physicochemical Characterization ◽  
Delivery Systems ◽  
Lipid Interactions

Formulation, Development and Characterization of Floating Beads of Diltiazem Hydrochloride

2016 ◽  
Vol 6 (1) ◽  
Author(s):  
Anamika Saxena Saxena ◽  
Santosh Kitawat ◽  
Kalpesh Gaur ◽  
Virendra Singh
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery Systems ◽  
Entrapment Efficiency ◽  
Repeated Administration ◽  
Alginate Beads ◽  
Delivery Systems ◽  
Sem Analysis ◽  
Formulation Development

The main goal of any drug delivery system is to achieve desired concentration of the drug in blood or tissue, which is therapeutically effective and nontoxic for a prolonged period. Various attempts have been made to develop gastroretentive delivery systems such as high density system, swelling, floating system. The recent developments of FDDS including the physiological and formulation variables affecting gastric retention, approaches to design single-unit and multiple-unit floating systems, and their classification and formulation aspects are covered in detail. Gastric emptying is a complex process and makes in vivo performance of the drug delivery systems uncertain. In order to avoid this variability, efforts have been made to increase the retention time of the drug-delivery systems for more than 12 hours. The floating or hydrodynamically controlled drug delivery systems are useful in such application. Background of the research: Diltiazem HCL (DTZ), has short biological half life of 3-4 h, requires rather high frequency of administration. Due to repeated administration there may be chances of patient incompliance and toxicity problems. Objective: The objective of study was to develop sustained release alginate beads of DTZ for reduction in dosing frequency, high bioavailability and better patient compliance. Methodology: Five formulations prepared by using different drug to polymer ratios, were evaluated for relevant parameters and compared. Alginate beads were prepared by ionotropic external gelation technique using CaCl2 as cross linking agent. Prepared beads were evaluated for % yield, entrapment efficiency, swelling index in 0.1N HCL, drug release study and SEM analysis. In order to improve %EE and drug release, LMP and sunflower oil were used as copolymers along with sodium alginate.

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.

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