Antibacterial Porous Coaxial Drug-Carrying Nanofibers for Sustained Drug-Releasing Applications

The phenomenon of drug burst release is the main problem in the field of drug delivery systems, as it means that a good therapeutic effect cannot be acheived. Nanofibers developed by electrospinning technology have large specific surface areas, high porosity, and easily controlled morphology. They are being considered as potential carriers for sustained drug release. In this paper, we obtained polycaprolactone (PCL)/polylactic acid (PLA) core-shell porous drug-carrying nanofibers by using coaxial electrospinning technology and the nonsolvent-induced phase separation method. Roxithromycin (ROX), a kind of antibacterial agent, was encapsulated in the core layer. The morphology, composition, and thermal properties of the resultant nanofibers were characterized by scanning electron microscopy (SEM), attenuated total reflection Fourier transform infrared (ATR-FTIR) spectroscopy, differential scanning calorimetry (DSC) and thermogravimetry analysis (TGA). Besides this, the in vitro drug release profile was investigated; it showed that the release rate of the prepared coaxial porous nanofibers with two different pore sizes was 30.10 ± 3.51% and 35.04 ± 1.98% in the first 30 min, and became 92.66 ± 3.13% and 88.94 ± 1.58% after 14 days. Compared with the coaxial nonporous nanofibers and nanofibers prepared by uniaxial electrospinning with or without pores, the prepared coaxial porous nanofibers revealed that the burst release was mitigated and the dissolution rate of the hydrophobic drugs was increased. The further antimicrobial activity demonstrated that the inhibition zone diameter of the coaxial nanofibers with two different pore sizes was 1.70 ± 0.10 cm and 1.73 ± 0.23 cm, exhibiting a good antibacterial effect against Staphylococcus aureus. Therefore, the prepared nanofibers with the coaxial porous structures could serve as promising drug delivery systems.

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Towards feedback-controlled nanomedicines for smart, adaptive delivery

Experimental Biology and Medicine ◽

10.1177/1535370218800456 ◽

2018 ◽

Vol 244 (4) ◽

pp. 283-293 ◽

Cited By ~ 4

Author(s):

Stephen J. Jones ◽

Annette F. Taylor ◽

Paul A Beales

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Drug Delivery Systems ◽

Delivery Systems ◽

The Body ◽

Living Systems ◽

Prolonged Release ◽

Drug Bioavailability ◽

Drug Release Profile ◽

Chemical Systems

Nanomedicines for controlled drug release provide temporal and spatial regulation of drug bioavailability in the body. The timing of drug release is usually engineered either for slow gradual release over an extended period of time or for rapid release triggered by a specific change in its physicochemical environment. However, between these two extremes, there is the desirable possibility of adaptive nanomedicines that dynamically modulate drug release in tune with its changing environment. Adaptation and response through communication with its environment is a fundamental trait of living systems; therefore, the design of biomimetic nanomedicines through the approaches of bottom-up synthetic biology provides a viable route to this goal. This could enable drug delivery systems to optimize release in synchronicity with the body’s natural biological rhythms and the personalized physiological characteristics of the patient, e.g. their metabolic rate. Living systems achieve this responsiveness through feedback-controlled biochemical processes that regulate their functional outputs. Towards this goal of adaptive drug delivery systems, we review the general benefits of nanomedicine formulations, provide existing examples of experimental nanomedicines that encapsulate the metabolic function of enzymes, and give relevant examples of feedback-controlled chemical systems. These are the underpinning concepts that hold promise to be combined to form novel adaptive release systems. Furthermore, we motivate the advantages of adaptive release through chronobiological examples. By providing a brief review of these topics and an assessment of the state of the art, we aim to provide a useful resource to accelerate developments in this field. Impact statement The timing and rate of release of pharmaceuticals from advanced drug delivery systems is an important property that has received considerable attention in the scientific literature. Broadly, these mostly fall into two classes: controlled release with a prolonged release rate or triggered release where the drug is rapidly released in response to an environmental stimulus. This review aims to highlight the potential for developing adaptive release systems that more subtlety modulate the drug release profile through continuous communication with its environment facilitated through feedback control. By reviewing the key elements of this approach in one place (fundamental principles of nanomedicine, enzymatic nanoreactors for medical therapies and feedback-controlled chemical systems) and providing additional motivating case studies in the context of chronobiology, we hope to inspire innovative development of novel “chrononanomedicines.”

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FORMULATION, DEVELOPMENT AND CHARACTERIZATION OF DRUG DELIVERY SYSTEMS BASED TELMISARTAN ENCAPSULATED IN SILK FIBROIN NANOSPHERE’S

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2019v11i1.30588 ◽

2019 ◽

Vol 11 (1) ◽

pp. 247 ◽

Cited By ~ 1

Author(s):

Shahid Ud Din Wani ◽

Gangadharappa H. V. ◽

Ashish N. P.

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Zeta Potential ◽

Silk Fibroin ◽

Drug Delivery Systems ◽

Delivery Systems ◽

Water Soluble ◽

Random Coil ◽

Burst Release

Objective: The aim of the present work was to formulate silk fibroin (SF) nanospheres (NS’s) for drug delivery application. The current study was designed to advance the water solubility and bio-availability of telmisartan by nanoprecipitation method.Methods: SF NS’s loaded with TS were prepared by nanoprecipitation method. The drug was dissolved in aqueous solution of SF by using acetone as a non-solvent. The prepared NS’s were then characterized by FTIR, X-ray diffraction and zeta potential, and were evaluated for its, surface morphology, %drug content, encapsulation efficiency and in vitro drug release.Results: The evaluation results of SF NS’s loaded of TS showed 74.22±0.17 % entrapment efficiency, 35.21±0.02 % of drug loading, and-4.9 mV to-13.6 mV of zeta potential due to the proper bounding of TS with the β-sheets of SF, the particle size reported was within the size range of 160-186 nm having smooth surface and were spherical in shape. The SFNS’s pattern switched from random coil to β-sheet formation on treating with acetone. FTIR and DSC studies marked no such inter-molecular interactions between SF and drug molecules. The % cumulative in vitro drug release from SF NS’s exhibited quick burst release. The in vitro cumulative drug release of SF NS’s of TS it was found that about 74% of the drug was released within 8 h and about 96% of drug released at 24 hr. The rate of drug release increased with the increase in SF ratio.Conclusion: It is believed that these SF NS’s will find potential applications in drug delivery release as drug carriers, especially poor water-soluble drugs. All these results proposed that SF NS’s are eventuality handy in various drug delivery systems.

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Remote Temperature-Responsive Parafilm Dermal Patch for On-Demand Topical Drug Delivery

Micromachines ◽

10.3390/mi12080975 ◽

2021 ◽

Vol 12 (8) ◽

pp. 975

Author(s):

Shahrukh Zaman Akash ◽

Farjana Yesmin Lucky ◽

Murad Hossain ◽

Asim Kumar Bepari ◽

G. M. Sayedur Rahman ◽

...

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Drug Delivery Systems ◽

Drug Carriers ◽

Delivery Systems ◽

Burst Release ◽

Therapeutic Effects ◽

Microbial Infection ◽

Temperature Responsive ◽

On Demand

The development of externally controlled drug delivery systems that can rapidly trigger drug release is widely expected to change the landscape of future drug carriers. In this study, a drug delivery system was developed for on-demand therapeutic effects. The thermoresponsive paraffin film can be loaded on the basis of therapeutic need, including local anesthetic (lidocaine) or topical antibiotic (neomycin), controlled remotely by a portable mini-heater. The application of mild temperature (45 °C) to the drug-loaded paraffin film allowed a rapid stimulus response within a short time (5 min). This system exploits regular drug release and the rapid generation of mild heat to trigger a burst release of 80% within 6 h of any locally administered drug. The in vitro drug release studies and in vivo therapeutic activity were observed for local anesthesia and wound healing using a neomycin-loaded film. The studies demonstrated on-demand drug release with minimized inflammation and microbial infection. This temperature-responsive drug-loaded film can be triggered remotely to provide flexible control of dose magnitude and timing. Our preclinical studies on these remotely adjustable drug delivery systems can significantly improve patient compliance and medical practice.

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A comprehensive review on polymeric micelles: a promising drug delivery carrier

Journal of Analytical & Pharmaceutical Research ◽

10.15406/japlr.2021.10.00372 ◽

2021 ◽

Vol 10 (3) ◽

pp. 102-107

Author(s):

Ajay Kumar

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Drug Delivery Systems ◽

Polymeric Micelles ◽

Delivery Systems ◽

Hydrophobic Drug ◽

Drug Release Profile ◽

Physiological Conditions ◽

Drug Molecules ◽

Drug Delivery Carrier

The main aim of drug delivery systems is to regulate the rate of drug release as per the patient's physiological conditions as well as the progression of the illness or as per the circadian rhythms. To achieve such objectives, the new drug delivery systems have been developed to provide the drug release profile, which is based on each patient's needs. Different researches have been done to create drug delivery carriers, focusing on targeting and delivering hydrophobic drug molecules. This review focuses on Polymeric Micelles as the promising drug delivery carrier due to its high stability, protective property against the harsh gastrointestinal environment.

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Mucoadhesive Formulation Designs for Oral Controlled Drug Release at the Colon

Current Pharmaceutical Design ◽

10.2174/1381612826666200917143816 ◽

2020 ◽

Vol 26 ◽

Author(s):

Phuong H.L. Tran ◽

Thao T.D. Tran

Keyword(s):

Drug Delivery ◽

Controlled Release ◽

Drug Release ◽

Basic Principle ◽

Oral Delivery ◽

Drug Delivery Systems ◽

Controlled Drug Release ◽

Delivery Systems ◽

Sustained Drug Release ◽

Mucosal Tissues

: Mucoadhesive formulations have been demonstrated to result in efficient drug delivery systems with advantages over existing systems such as increased local retention and sustained drug release via adhesiveness to mucosal tissues. The controlled release of colon-targeted, orally administered drugs has recently attracted a number of studies investigating mucoadhesive systems. Consequently, substantial designs, from mucoadhesive cores to shells of particles, have been studied with promising applications. This review will provide an overview of and discuss specific strategies for developing mucoadhesive systems for colon-targeted oral delivery with controlled drug release, including mucoadhesive matrices, cross-linked mucoadhesive microparticles, coatings and mucoadhesive nanoparticles. The understanding of the basic principle of these designs and advanced formulations throughout will lead to the development of products with efficient drug delivery at the colon for therapies for different diseases.

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On-Demand Drug Delivery Systems Using Nanofibers

Nanomaterials ◽

10.3390/nano11123411 ◽

2021 ◽

Vol 11 (12) ◽

pp. 3411

Author(s):

Baljinder Singh ◽

Kibeom Kim ◽

Myoung-Hwan Park

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Drug Delivery Systems ◽

Target Location ◽

Release Kinetics ◽

Drug Loading ◽

Delivery Systems ◽

Therapeutic Effects ◽

High Porosity ◽

On Demand

On-demand drug-delivery systems using nanofibers are extensively applicable for customized drug release based on target location and timing to achieve the desired therapeutic effects. A nanofiber formulation is typically created for a certain medication and changing the drug may have a significant impact on the release kinetics from the same delivery system. Nanofibers have several distinguishing features and properties, including the ease with which they may be manufactured, the variety of materials appropriate for processing into fibers, a large surface area, and a complex pore structure. Nanofibers with effective drug-loading capabilities, controllable release, and high stability have gained the interest of researchers owing to their potential applications in on-demand drug delivery systems. Based on their composition and drug-release characteristics, we review the numerous types of nanofibers from the most recent accessible studies. Nanofibers are classified based on their mechanism of drug release, as well as their structure and content. To achieve controlled drug release, a suitable polymer, large surface-to-volume ratio, and high porosity of the nanofiber mesh are necessary. The properties of nanofibers for modified drug release are categorized here as protracted, stimulus-activated, and biphasic. Swellable or degradable polymers are commonly utilized to alter drug release. In addition to the polymer used, the process and ambient conditions can have considerable impacts on the release characteristics of the nanofibers. The formulation of nanofibers is highly complicated and depends on many variables; nevertheless, numerous options are available to accomplish the desired nanofiber drug-release characteristics.

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Formulation, Development and Characterization of Floating Beads of Diltiazem Hydrochloride

International Journal of Drug Delivery Technology ◽

10.25258/ijddt.v6i1.8883 ◽

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.

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Improving the Efficacy of Anticancer Drugs via Encapsulation and Acoustic Release

Current Topics in Medicinal Chemistry ◽

10.2174/1568026618666180608125344 ◽

2018 ◽

Vol 18 (10) ◽

pp. 857-880 ◽

Cited By ~ 3

Author(s):

Salma E. Ahmed ◽

Nahid Awad ◽

Vinod Paul ◽

Hesham G. Moussa ◽

Ghaleb A. Husseini

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Drug Delivery Systems ◽

Delivery Systems ◽

Special Focus ◽

Nano Drug Delivery ◽

Medical Researchers ◽

History Of ◽

Overall Performance ◽

Enhanced Stability

Conventional chemotherapeutics lack the specificity and controllability, thus may poison healthy cells while attempting to kill cancerous ones. Newly developed nano-drug delivery systems have shown promise in delivering anti-tumor agents with enhanced stability, durability and overall performance; especially when used along with targeting and triggering techniques. This work traces back the history of chemotherapy, addressing the main challenges that have encouraged the medical researchers to seek a sanctuary in nanotechnological-based drug delivery systems that are grafted with appropriate targeting techniques and drug release mechanisms. A special focus will be directed to acoustically triggered liposomes encapsulating doxorubicin.

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Nanostructured Ketorolac-Tromethamine/MCF: Synthesis, Characterization and Application in Drug Release System

Current Nanoscience ◽

10.2174/1573413714666180222134742 ◽

2018 ◽

Vol 14 (5) ◽

pp. 432-439 ◽

Cited By ~ 1

Author(s):

Juliana M. Juarez ◽

Jorgelina Cussa ◽

Marcos B. Gomez Costa ◽

Oscar A. Anunziata

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Therapeutic Efficacy ◽

Drug Delivery Systems ◽

Controlled Drug Release ◽

Delivery Systems ◽

The Body ◽

Fickian Diffusion ◽

Ketorolac Tromethamine

Background: Controlled drug delivery systems can maintain the concentration of drugs in the exact sites of the body within the optimum range and below the toxicity threshold, improving therapeutic efficacy and reducing toxicity. Mesostructured Cellular Foam (MCF) material is a new promising host for drug delivery systems due to high biocompatibility, in vivo biodegradability and low toxicity. Methods: Ketorolac-Tromethamine/MCF composite was synthesized. The material synthesis and loading of ketorolac-tromethamine into MCF pores were successful as shown by XRD, FTIR, TGA, TEM and textural analyses. Results: We obtained promising results for controlled drug release using the novel MCF material. The application of these materials in KETO release is innovative, achieving an initial high release rate and then maintaining a constant rate at high times. This allows keeping drug concentration within the range of therapeutic efficacy, being highly applicable for the treatment of diseases that need a rapid response. The release of KETO/MCF was compared with other containers of KETO (KETO/SBA-15) and commercial tablets. Conclusion: The best model to fit experimental data was Ritger-Peppas equation. Other models used in this work could not properly explain the controlled drug release of this material. The predominant release of KETO from MCF was non-Fickian diffusion.

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