Stimuli-Responsive Capsule Membranes for Controlled Release in Pharmaceutical Applications

2017 ◽  
Vol 23 (2) ◽  
pp. 295-301 ◽  
Author(s):  
Zhuang Liu ◽  
Xiao-Jie Ju ◽  
Wei Wang ◽  
Rui Xie ◽  
Lu Jiang ◽  
...  
Keyword(s):  
Controlled Release ◽  
Drug Concentration ◽  
Drug Carriers ◽  
Burst Release ◽  
Stimuli Responsive ◽  
Pharmaceutical Applications ◽  
Conventional Drug ◽  
Controllable Release ◽  
Capsule Size

Background: In conventional drug delivery, the drug concentration in the blood raises once the drug taken, and then peaks and declines. Since each drug has a level above which it is toxic and another level below which it is ineffective, the drug concentration in a patient at a particular time depends on compliance with the prescribed routine. Methods: To achieve more effective efficacy and fewer side effects of drugs, the drug carriers with desirable dosing and controllable release property of drugs are highly desired. Stimuli-responsive capsules with smart gating membranes or hydrogel-based membranes as capsule shells are ideal candidates. The smart capsule membranes enable efficient encapsulation of drugs within the large inner volume, and the responsive gating membranes or hydrogel-based membranes could control the release rate of encapsulated drugs in responding to environmental stimuli. The trigger stimuli could be either artificial or natural ones corresponding to specific diseases, such as temperature, pH, glucose concentration, specific ion, light, and magnetic field. Results: This review highlights the recent development in stimuli-responsive capsule membranes for controlled release in pharmaceutical applications, including two types of stimuli-responsive capsule membranes with different architectures for on/off release and burst release, which can achieve potential uses of case-dependent on/off release and burst release. Conclusion: The preponderances of the smart capsule membranes are that the capsules are with controllable inner space for drug vehicles with desired dose and stimuli-responsive membrane as shell to release drugs at a desired site and/or moment. However, the actual difficulties for the stimuli-responsive capsule membrane systems to go before they can be applied widely in the biomedical fields are discussed. The future works should focus on the improvements of biocompatibility, biodegradability and stimuli-responsiveness of the capsule membranes, easy and scalable fabrication techniques with further decrease of the capsule size for more efficient in vivo applications, and the diversification of the multi-compartmental capsule architectures with multi-stimuli-responsive characteristics for controlled release.

Stimuli-responsive Carriers for Controlled Intracellular Drug Release

2019 ◽  
Vol 26 (13) ◽  
pp. 2377-2388 ◽  
Author(s):  
Yan Sheng ◽  
Jiaming Hu ◽  
Junfeng Shi ◽  
Ly James Lee
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Redox Potential ◽  
Drug Carriers ◽  
Therapeutic Agents ◽  
Stimuli Responsive ◽  
Recent Developments ◽  
Disease Site ◽  
Catalyzed Reactions ◽  
Enzyme Catalyzed Reactions

Background: Stimuli-responsive carriers are a class of drug delivery systems which can change their physicochemical properties and/or structural conformations in response to specific stimuli. Although passive and active drug targeting has proved to reduce the side effects to normal cells, controlled intracellular drug release should be included in drug carriers to enhance the bioavailability of drugs at the disease site. Methods: This review focuses on several recent advances in the development of stimuli-responsive carriers for spatially and temporally controlled release of therapeutic agents in response to intracellular stimuli, such as pH, redox potential, reactive oxygen species, enzyme and temperature. Results: Among the different types of stimuli, pH-responsive carriers have been mostly used to design intracellular controlled release system. The sharp difference of redox potential between inside and outside cells is attributed to the high variation in concentration of glutathione. ROS-responsive carriers are gaining much attention for selective release of therapeutic agents by sensing oxidative conditions at different levels. The advantages of utilizing enzymes as the trigger of stimuli-responsive carriers include diverse types of enzymes, high selectivity of enzyme catalyzed reactions and the mild reaction conditions involved. Abnormal temperature is another unique stimulus and has been widely used to trigger controlled release of drug in tumor cells. Conclusion: Recent developments highlighted in this paper demonstrate that stimuli-responsive carriers possess great potential as a new platform for controlled intracellular drug release.

scholarly journals Fabrication and application of dimyristoyl phosphatidylcholine biomaterial-based nanocochleates dry powder inhaler for controlled release resveratrol delivery

2021 ◽  
Vol 7 (1) ◽  
Author(s):  
A. J. Mali ◽  
P. A. Joshi ◽  
C. Bothiraja ◽  
A. P. Pawar
Keyword(s):  
Particle Size ◽  
Controlled Release ◽  
Respiratory Diseases ◽  
Dry Powder Inhaler ◽  
Albino Rats ◽  
Burst Release ◽  
Dry Powder ◽  
In Vivo Toxicity ◽  
Chronic Respiratory Diseases

Abstract Background Resveratrol, a bioactive phytoconstituent, is used to treat chronic respiratory diseases. However, its clinical application was hampered due to its poor bioavailability. In the present study, controlled release of resveratrol loaded nanocochleate-based dry powder inhaler was investigated to improve its biopharmaceutical properties for pulmonary drug delivery. The in vivo toxicity study was performed in the healthy male albino Wistar rats by intracheal administration. Results Resveratrol loaded nanocochleate-based dry powder inhaler was prepared by lyophilizing the resveratrol loaded dimyristoylphosphatidylcholine sodium and calcium ion-based nanocochleates using mannitol as cryoprotectant. Resveratrol loaded nanocochleates showed a particle size and encapsulation efficiency of 329.18 ± 9.43 nm and 76.35 ± 3.65%, respectively. Resveratrol loaded nanocochleate-based dry powder exhibited a particle size of 102.21 ± 9.83 μm and satisfactory flowability with initial burst release followed by extended release up to 96 h. The in vitro drug deposition pattern using multistage cascade impactor showed 1.28-fold improvement in fine particle dose, and the in vivo toxicity potential by histopathological study in albino rats revealed safety of formulation. Conclusions Resveratrol loaded nanocochleate-based dry powder inhaler could serve as an efficient delivery system for the treatment of chronic respiratory diseases. Graphical abstract

Polymeric micelles for anticancer drug delivery

2020 ◽  
Vol 11 (10) ◽  
pp. 613-635 ◽  
Author(s):  
Nairrita Majumder ◽  
Nandita G Das ◽  
Sudip K Das
Keyword(s):  
Drug Delivery ◽  
Polymeric Micelles ◽  
Clinical Status ◽  
Cancer Therapeutics ◽  
Stimuli Responsive ◽  
Anticancer Drug Delivery ◽  
Properties And Characterization ◽  
Conventional Drug ◽  
Recent Developments

Polymeric micelles have gained interest as novel drug delivery systems for the treatment and diagnosis of cancer, as they offer several advantages over conventional drug therapies. This includes drug targeting to tumor tissue, in vivo biocompatibility and biodegradability, prolonged circulation time, enhanced accumulation, retention of the drug loaded micelle in the tumor and decreased side effects. This article provides an overview on the current state of micellar formulations as nanocarriers for anticancer drugs and their effectiveness in cancer therapeutics, including their clinical status. The type of copolymers used, their physicochemical properties and characterization as well as recent developments in the design of functional polymeric micelles are highlighted. The article also presents the design and outcomes of various types of stimuli-responsive polymeric micelles.

scholarly journals Controlled Delivery of Pan-PAD-Inhibitor Cl-Amidine Using Poly(3-Hydroxybutyrate) Microspheres

2021 ◽  
Vol 22 (23) ◽  
pp. 12852
Author(s):  
Dina Ahmed ◽  
Hima Puthussery ◽  
Pooja Basnett ◽  
Jonathan C. Knowles ◽  
Sigrun Lange ◽  
...  
Keyword(s):  
Controlled Release ◽  
Release Kinetics ◽  
Chemotherapeutic Agents ◽  
Lower Amount ◽  
Burst Release ◽  
Vegf Expression ◽  
In Vivo Models ◽  
Anti Cancer

This study deals with the process of optimization and synthesis of Poly(3-hydroxybutyrate) microspheres with encapsulated Cl-amidine. Cl-amidine is an inhibitor of peptidylarginine deiminases (PADs), a group of calcium-dependent enzymes, which play critical roles in a number of pathologies, including autoimmune and neurodegenerative diseases, as well as cancer. While Cl-amidine application has been assessed in a number of in vitro and in vivo models; methods of controlled release delivery remain to be investigated. P(3HB) microspheres have proven to be an effective delivery system for several compounds applied in antimicrobial, wound healing, cancer, and cardiovascular and regenerative disease models. In the current study, P(3HB) microspheres with encapsulated Cl-amidine were produced in a size ranging from ~4–5 µm and characterized for surface morphology, porosity, hydrophobicity and protein adsorption, in comparison with empty P(3HB) microspheres. Cl-amidine encapsulation in P(3HB) microspheres was optimized, and these were found to be less hydrophobic, compared with the empty microspheres, and subsequently adsorbed a lower amount of protein on their surface. The release kinetics of Cl-amidine from the microspheres were assessed in vitro and expressed as a function of encapsulation efficiency. There was a burst release of ~50% Cl-amidine in the first 24 h and a zero order release from that point up to 16 days, at which time point ~93% of the drug had been released. As Cl-amidine has been associated with anti-cancer effects, the Cl-amidine encapsulated microspheres were assessed for the inhibition of vascular endothelial growth factor (VEGF) expression in the mammalian breast cancer cell line SK-BR-3, including in the presence of the anti-proliferative drug rapamycin. The cytotoxicity of the combinatorial effect of rapamycin with Cl-amidine encapsulated P(3HB) microspheres was found to be 3.5% more effective within a 24 h period. The cells treated with Cl-amidine encapsulated microspheres alone, were found to have 36.5% reduction in VEGF expression when compared with untreated SK-BR-3 cells. This indicates that controlled release of Cl-amidine from P(3HB) microspheres may be effective in anti-cancer treatment, including in synergy with chemotherapeutic agents. Using controlled drug-delivery of Cl-amidine encapsulated in Poly(3-hydroxybutyrate) microspheres may be a promising novel strategy for application in PAD-associated pathologies.

scholarly journals Design and in vivo Evaluation of Controlled Release Gliclazide Trilayer Matrix Tablets in the Management of Diabetes Mellitus

2018 ◽  
Vol 10 (05) ◽  
Author(s):  
D.V.R.N. Bhikshapathi ◽  
B. Ram Prasad
Keyword(s):  
Diabetes Mellitus ◽  
Plasma Concentration ◽  
Controlled Release ◽  
Drug Release ◽  
Drug Concentration ◽  
Hydroxypropyl Methylcellulose ◽  
Physicochemical Characteristics ◽  
Matrix Tablets ◽  
Dissolution Profile

The purpose of the present study was to develop and optimize multi-layered matrix tablets of Gliclazide trilayer tablets to achieve zero-order drug release for sustained plasma concentration. Gliclazide tablets were prepared by direct compression and consist of middle active layer with different grades of hydroxypropyl methylcellulose (HPMC K 4M, K 15M and K100M), Guar gum and Eudragit L 100. The tablets were also evaluated for physicochemical characteristics and release kinetics. The physicochemical characteristics of the prepared tablets were satisfactory. The developed drug delivery systems showed prolonged drug release rates over a period of 24 h. In vivo bioavailability studies were carried out on the optimized formulation (EF14), mean time to attain peak drug concentration (Tmax) was 6.00 ± 0.14 and 4.02 ± 0.12 h for the optimized and marketed product respectively, while mean maximum drug concentration (Cmax) was 124.80 ± 1.02 ng/ml and 95.12 ± 1.05 ng/ml respectively. AUC0-α and AUC0-t for optimized formulation was significantly higher (p less than 0.05) as compared to marketed product. A fair correlation between the dissolution profile and bioavailability for the optimized formulation was observed. The results indicate that the approach used could lead to a successful development of a controlled release formulation of the drug. The EF14 was shown significant plasma concentration with controlled release and maintained for 24 hours with patient compliance by reducing the dosage frequency, when compared with marketed product in the efficient management of Diabetes mellitus.

Hydrated Polymer System as Efficient Carrier for the Delivery of Drugs Against Viral Infections

2015 ◽  
Vol 5 (2) ◽  
Author(s):  
Cinu Jacob ◽  
Ramya D. ◽  
Vedha B.N.
Keyword(s):  
Drug Delivery ◽  
Controlled Release ◽  
Drug Delivery Systems ◽  
Suspension Polymerization ◽  
Polymer System ◽  
Drug Carriers ◽  
Delivery Systems ◽  
Aqueous Environment ◽  
Burst Release ◽  
Specific Response

Hydrogels are crosslinked polymers which has the ability to absorb water in aqueous media.Hydrogels are being prepared by different methods such as suspension polymerization, chemical or physical crosslinking, solution polymerization, radiation polymerization etc., and using different types of polymers. Hydrogels exhibiting swelling mechanism have been extensively used as drug carriers in the controlled drug delivery systems. The wide application of these biomaterials is due to its characteristics such as swelling in the aqueous environment, specific response to the pH, temperature, ion, electric stimuli sensitivity etc., Hydrogels of biocompatible polymers have good loading capacity and so widely used for the encapsulation of drugs which can be targeted to the specific sites. Since the rate of drug diffusion from hydrogels can be controlled, these materials are potentially useful as drug delivery systems. Controlled release of many drugs including anticancer and antiviral agents has been efficiently done using hydrogels. Especially various anti-HIV drugs have been successfully formulated as hydrogel systems for the controlled release and prolonged action. Bilayer and multilayer hydrogels have grown importance in recent days, wherein a burst release followed by controlled release could be achieved for superior therapeutic action at reduced dose and side effects. Also the efficiency of incorporating more than one drug in different layers of hydrogels is being investigated to improve combination therapy for various disorders.

Bioinspired Polymeric-based Core-shell Smart Nano-systems

2019 ◽  
Vol 7 (3) ◽  
pp. 181-205 ◽  
Author(s):  
Ranjit K. Harwansh ◽  
Rohitas Deshmukh ◽  
Md Abul Barkat ◽  
Md. Akhlaquer Rahman
Keyword(s):  
Drug Delivery ◽  
Smart Materials ◽  
Drug Loading ◽  
Physicochemical Characterization ◽  
Bioactive Molecules ◽  
Burst Release ◽  
Therapeutic Effects ◽  
Stimuli Responsive ◽  
Engineering Technology ◽  
Conventional Drug

Smart nanosystems (SNs) have the potential to revolutionize drug delivery. Conventional drug delivery systems have poor drug-loading, early burst release, limited therapeutic effects, etc. Thus, to overcome these problems, researchers have taken advantage of the host-guest interactions as bioinspired nanosystems which can deliver nanocarriers more efficiently with the maximum drug loading capacity and improved therapeutic efficacy as well as bioavailability. SNs employ nanomaterials to form cage molecules by entrapping new nanocarriers called smart nanosystems in their cargo and design. The activities of SNs are based on responsive materials that interact with the stimuli either by changing their properties or conformational structures. The aptitude of living systems to respond to stimuli and process information has encouraged researchers to build up integrated nanosystems exhibiting similar function and therapeutic response. Various smart materials, including polymers, have been exhaustively employed in fabricating different stimuli-responsive nanosystems which can deliver bioactive molecules to a specific site for a certain period with minimal side effects. SNs have been widely explored to deliver diverse kinds of therapeutic agents ranging from bioactive compounds, genes, and biopharmaceuticals like proteins and peptides, to diagnostic imaging agents for biomedical applications. Nanotechnology-based different nanosystems are promising for health care issues. The advancement of SNs with physical science and engineering technology in synthesizing nanostructures and their physicochemical characterization should be exploited in medicine and healthcare for reducing mortality rate, morbidity, disease prevalence and general societal burden.

scholarly journals Stimuli-Responsive Poly(aspartamide) Derivatives and Their Applications as Drug Carriers

2021 ◽  
Vol 22 (16) ◽  
pp. 8817
Author(s):  
Guangyan Zhang ◽  
Hui Yi ◽  
Chenhui Bao
Keyword(s):  
Amino Acid ◽  
Controlled Release ◽  
Physical Properties ◽  
Drug Loading ◽  
Drug Carriers ◽  
Stimuli Responsive ◽  
External Stimuli

Poly(aspartamide) derivatives, one kind of amino acid-based polymers with excellent biocompatibility and biodegradability, meet the key requirements for application in various areas of biomedicine. Poly(aspartamide) derivatives with stimuli-responsiveness can usually respond to external stimuli to change their chemical or physical properties. Using external stimuli such as temperature and pH as switches, these smart poly(aspartamide) derivatives can be used for convenient drug loading and controlled release. Here, we review the synthesis strategies for preparing these stimuli-responsive poly(aspartamide) derivatives and the latest developments in their applications as drug carriers.

scholarly journals Tumor Cell Distinguishable Nanomedicine Integrating Chemotherapeutic Sensitization and Protection

2021 ◽  
Vol 9 ◽  
Author(s):  
Sen Liu ◽  
Can Shen ◽  
Cheng Qian ◽  
Jianquan Wang ◽  
Zhongmei Yang ◽  
...  
Keyword(s):  
Controlled Release ◽  
Near Infrared ◽  
Electron Excitation ◽  
Drug Dosage ◽  
Burst Release ◽  
Normal Cells ◽  
Chemotherapy Drugs ◽  
Transfer Group

Theoretically, with a high enough drug dosage, cancer cells could be eliminated. However, the dosages that can be administered are limited by the therapeutic efficacy and side effects of the given drug. Herein, a nanomedicine integrating chemotherapeutic sensitization and protection was developed to relieve the limitation of administration dosage and to improve the efficacy of chemotherapy. The nanomedicine was endowed with the function of synergistically controlled release of CO and drugs under near-infrared (NIR) light irradiation. CO photo-induced release system (COPIRS) was synthesized by constructing an electron excitation–electron transfer group–electron-induced CO release structure and was used as the hydrophobic part, and then hydrophilic polymer (polyethylene glycol; PEG) was introduced by a thermal-responsive groups (DA group), forming a near-infrared-induced burst-release nanocarrier. In vitro and in vivo experiments showed that the nanomedicine can distinguish between tumor and normal cells and regulates the resistance of these different cells through the controlled release of carbonic oxide (CO), simultaneously enhancing the efficacy of chemotherapy drugs on tumor cells and chemotherapeutic protection on normal cells. This strategy could solve the current limitations on dosages due to toxicity and provide a solution for tumor cure by chemotherapy.

Nanodrugs as a new approach in therapy of cardiovascular diseases and cancer with tumor-associated angiogenesis

2020 ◽  
Vol 28 ◽  
Author(s):  
Justyna Hajtuch ◽  
Karolina Niska ◽  
Iwona Inkielewicz-Stepniak
Keyword(s):  
Cardiovascular Disease ◽  
Cardiovascular Diseases ◽  
Controlled Drug Release ◽  
Biological Properties ◽  
Comprehensive Information ◽  
Conventional Drug ◽  
Key Factor ◽  
Functionalized Materials

Background: Cancer along with cardiovascular diseases are globally defined as leading causes of death. Importantly, some risk factors are common to these diseases. The process of angiogenesis and platelets aggregation are observed in cancer development and progression. In recent years, studies have been conducted on nanodrugs in these diseases that have provided important information on the biological and physicochemical properties of nanoparticles. Their attractive features are that they are made of biocompatible, well-characterized and easily functionalized materials. Unlike conventional drug delivery, sustained and controlled drug release can be obtained by using nanomaterials. Methods: In this article, we review the latest research to provide comprehensive information on nanoparticle-based drugs for the treatment of cancer, cardiovascular disease associated with abnormal haemostasis, and the inhibition of tumorassociated angiogenesis. Results: The results of the analysis of data based on nanoparticles with drugs confirm their improved pharmaceutical and biological properties, which gives promising antiplatelet, anticoagulant and antiangiogenic effects. Moreover, the review included in vitro, in vivo research and presented nanodrugs with chemotherapeutics approved by Food and Drug Administration. Conclusion: By the optimization of nanoparticles size and surface properties, nanotechnology are able to deliver drugs with enhanced bioavailability in treatment of cardiovascular disease, cancer and inhibition of cancer-related angiogenesis. Thus, nanotechnology can improve the therapeutic efficacy of the drug, but there is a need for a better understanding of the nanodrugs interaction in the human body, because this is a key factor in the success of potential nanotherapeutics.

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