Drug Carrier For Controlled Release Research Articles

Preparation, Swelling, and Drug Release Studies of Chitosan-based Hydrogels for Controlled Delivery of Buspirone Hydrochloride.

Buspirone is used for the management of depression and anxiety disorders. Due to its short half-life and low bioavailability, it requires multiple daily doses and is associated with some side effects. This study aimed to develop chitosan-based hydrogels as drug-controlled release carriers. The objective of this study is to prepare chitosan-based hydrogels as controlled release carriers in order to overcome the side effects of buspirone HCl and improve patients' compliance and their life quality. Polymer chitosan was polymerized with two monomers, acrylic acid and itaconic acid, to synthesize pH-sensitive hydrogel. The Fourier transform infrared spectroscopy (FTIR), thermogravimetric analysis (TGA) and differential scanning calorimetry (DSC) analysis were performed to confirm the structure formation and thermal stability. Water penetration capability and loading of the drug were performed by porosity and drug loading studies. The swelling and dissolution tests were performed to analyze the pH-sensitive nature of the developed hydrogels. FTIR, TGA, and DSC demonstrated that the chitosan-based hydrogels were successfully prepared. An increase in water penetration and drug loading into the hydrogel network was seen with the high incorporation of chitosan, acrylic acid, and itaconic acid. The swelling and dissolution studies revealed that prepared hydrogel offered the greatest swelling and drug release at a high pH of 7.4. The swelling and drug release from the hydrogel were affected by the concentrations of the incorporated contents. A controlled release of the drug was achieved by using chitosan-based hydrogel as a delivery carrier compared to commercial tablets of buspirone. The results showed that the developed chitosan-based hydrogel can be considered one of the most suitable drug carrier systems for the controlled delivery of buspirone.

Hypoxia-responsive calixarene-grafted self-assembled peptide hydrogel for inflammation suppression in ischemic stroke

Hypoxia is a significant characteristic of ischemic stroke. Recently, development of the pathology of tissue injury and deployment of new hypoxia-responsive technologies provide further opportunity for the application of hypoxia-responsive materials beyond cancer. To fully take advantage of hypoxic pathological feature of stroke and make advancement of stroke therapy, a hypoxia-responsive self-assembled peptide hydrogel was prepared for inflammation suppression in ischemic stroke treatment, utilizing azocalixarene (CA) as a hypoxia-responsive controlled release drug carrier. After induction of PBS, the peptide hydrogel was fabricated with brain-similar rheological modulus and shear-thinning property. The hypoxia-responsive performance of the peptide hydrogel was validated by three hypoxia & reductase systems including sodium hydrosulfite (SDT), rat liver microsomes and oxygen-glucose deprivation model (OGD) to achieve the responsive release of Cyanine 5-dimethyl (CY5-DM) or Fingolimod (FTY720) in vitro. After local administration of the hypoxia-responsive self-assembled peptide hydrogel, the improved motor function, reduced infarct volume and alleviated inflammation were achieved, revealing the effective stroke therapy in vivo.

Synthesis and characterization of magnetic molecularly imprinted polymer of polydopamine/graphene oxide as drug carrier for rivastigmine

In this study, a magnetic molecularly imprinted polymer based on magnetic graphene oxide and polydopamine (PDA) was synthesized, and its application in a drug delivery system (DDS) for rivastigmine (RIV) was investigated. In order to investigate the effect of imprinting on the performance of the MIP-GO/Fe3O4/PDA, its non-imprinted polymer (NIP-GO/Fe3O4/PDA) was also synthesized. Various analyses such as Fourier transform infrared spectrometer (FT-IR), scanning electron microscopy (SEM), thermal gravimetric analysis (TGA), vibrating-sample magnetometer (VSM), N2 adsorption and desorption (Brunauer-Emmett-Teller, BET), energy dispersive X-ray analysis (EDX), and X-ray diffraction analysis (XRD) were used to characterize the prepared polymers. The isotherm and kinetics studies for the drug loading process were done and modeled by various models. Drug release was performed in buffers with different pHs of 2.2, 6.4, 7.4, and 9, and in addition, in simulated nasal electrolyte solution (SNES) buffer. In addition, to investigate the drug release mechanisms, different models were studied. The results of this study showed that the drug loading process in this polymer follows the Freundlich isotherm model and the pseud-second-order model. The maximum efficiency of drug loading on the MIP and NIP was 96.44% and 72.78% at 400 ppm drug concentration, respectively. The results of drug release by these two polymers showed that molecularly imprinted techniques caused controlled drug release carriers, and the maximum amount of drug released from this polymer was 78.65% (301.98 ppm) at pH 9. In addition, the results of drug release modeling showed that the mechanism of rivastigmine release from MIP-GO/Fe3O4/PDA is Fickian diffusion.

Hyaluronic Acid-Alginate Homogeneous Structures with Polylactide Coating Applied in Controlled Antibiotic Release.

The use of a controlled-release drug carrier is an innovative solution for the treatment of local infections, in particular in dentistry, skin diseases, and in open wounds. The biocompatibility, biodegradability, the possibility of a large amount of drug adsorbed (especially those with hydrophilic properties), and the ability to create structures of any shape and size are the reasons for hydrogels to be frequently studied. The main disadvantage of hydrogel carriers is the rapid rate of drug release; hence, in this study, an attempt was made to additionally chemically cross-link 1-ethyl-3-(3-dimethyl aminopropyl)-1-carbodiimide hydrochloride (EDC) with the hyaluronic acid-alginate (HA-SAL) structure. The answer to significantly reduce the mass flux typical for hydrogel structure was to surround it with a polymer layer using a dry cover. By coating the carriers with polylactide, the release time was increased by around forty times. As the carriers were designed to reduce local bacterial infections, among others in dentistry, the released antibiotics were amoxycillin, metronidazole, and doxycycline.

Development of polymeric microbeads-intercalated with montmorillonite nanoclay and silver nanoparticles for controlled release of levofloxacin, an antibacterial drug

Controlled release drug carriers have gained significant interest in recent years due to their potential to produce greater therapeutic success. To address this need, the study presents the fabrication of sodium alginate/poly(vinylpyrrolidone-co-vinyl acetate) microbeads intercalated with montmorillonite (MMT) clay and silver nanoparticles for the controlled release of levofloxacin by a simple ionotropic gelation technique. The prepared beads were characterized using Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), X-ray diffraction (X-RD), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA) etc. The antibacterial activities of the synthesized microbeads were tested against Escherichia coli and Bacillus cereus by the agar disc diffusion method. The developed microbeads could significantly inhibit bacterial development. In vitro release studies and swelling studies were carried out at pH 7.4 simulated intestinal fluid and pH 1.2 simulated gastric fluid at 25 oC and 37 oC. The MMT-containing microbeads showed higher encapsulation efficiency and controlled drug release than other formulations. The results obtained from the swelling and in vitro release studies revealed that pH had influenced the drug release of developed microbeads and that they are suitable for intestinal drug delivery. The in vitro release kinetics was assessed by fitting the release data into the Korsmeyer- Peppas equation and finding that the release mechanism follows the Fickian diffusion process.

Use of mesoporous polydopamine nanoparticles as a stable drug-release system alleviates inflammation in knee osteoarthritis.

Osteoarthritis drugs are often short-acting; therefore, to enhance their efficacy, long-term, stable-release, drug-delivery systems are urgently needed. Mesoporous polydopamine (MPDA), a natural nanoparticle with excellent biocompatibility and a high loading capacity, synthesized via a self-aggregation-based method, is frequently used in tumor photothermal therapy. Here, we evaluated its efficiency as a sustained and controlled-release drug carrier and investigated its effectiveness in retarding drug clearance. To this end, we used MPDA as a controlled-release vector to design a drug-loaded microsphere system (RCGD423@MPDA) for osteoarthritis treatment, and thereafter, tested the efficacy of the system in a rat model of osteoarthritis. The results indicated that at an intermediate drug-loading dose, MPDA showed high drug retention. Furthermore, the microsphere system maintained controlled drug release for over 28 days. Our in vitro experiments also showed that drug delivery using this microsphere system inhibited apoptosis-related cartilage degeneration, whereas MPDA-only administration did not show obvious cartilage degradation improvement effect. Results from an in vivo osteoarthritis model also confirmed that drug delivery via this microsphere system inhibited cartilage damage and proteoglycan loss more effectively than the non-vectored drug treatment. These findings suggest that MPDA may be effective as a controlled-release carrier for inhibiting the overall progression of osteoarthritis. Moreover, they provide insights into the selection of drug-clearance retarding vectors, highlighting the applicability of MPDA in this regard.

Acid-Degradable Hydrogen-Generating Metal-Organic Framework for Overcoming Cancer Resistance/Metastasis and Off-Target Side Effects.

The development of stimuli‐responsively degradable porous carriers for both controlled drug release and high biosafety is vitally important to their clinical translation, but still challenging at present. A new type of porphyrin–iron metal organic framework (Fe‐MOF) nanocrystals is engineered here as acid‐degradable drug carrier and hydrogen donor by the coordination between porphyrin and zero‐valence Fe atom. Fe‐MOF nanocrystals exhibit excellent acid‐responsive degradation for H2 generation and simultaneous release of the loaded drug for combined hydrogen‐chemotherapy of cancer multidrug resistance (MDR) and metastasis and for local hydrogen eradication of the off‐target induced toxic side effects of the drug to normal cells/tissues. Mechanistically, released H2 assists chemotherapeutic drug to efficiently inhibit cancer metastasis by immunoactivating intratumoral M1‐phenotype macrophages and consequently downregulating the expression of metastasis‐related matrix metalloproteinase‐2 (MMP‐2) and can also downregulate the expressions of both P‐glycoprotein (P‐gp) protein and adenosine triphosphate (ATP) in MDR cancer cells to sensitize chemotherapeutic drug for enhanced damage to mitochondria and DNA. High anti‐MDR/antimetastasis efficacies and high biocompatibility endow Fe‐MOF nanocrystals and the Fe‐MOF‐based nanomedicine with high potential for clinical translation.

Phosphoglyceride‐coated polylactic acid porous microspheres and its regulation of curcumin release behavior

AbstractPolymer microspheres are widely used as carriers in delivering of hydrophobic or hydrophilic drugs. Surface coating of microspheres could be one of the attractive strategies to improve their properties. In this study, biodegradable polymer polylactic acid was dissolved in chloroform and non‐solvent to electrospray porous polymer microspheres. The properties of the microspheres were improved by phosphoglyceride (P‐P‐Gly) coating, and its behavior was investigated by loading with curcumin as a model drug. The morphologies of different microspheres were observed by scanning electron microscope. The results indicated that the microspheres obtained by dimethyl sulfoxide as non‐solvent could form the structure with porous characteristics. X‐ray diffraction, X‐ray photoelectron spectroscopy, and Fourier transform infrared spectroscopy analysis revealed that P‐P‐Gly was successfully coated on the surface of the microspheres. In addition, the thermal behavior of the coated microspheres was investigated by differential scanning calorimetry. In vitro release experiments indicated that the drug‐loaded microspheres showed a very gentle release trend, which was mainly due to the P‐P‐Gly coating could not completely cover the pores of the microspheres. The P‐P‐Gly‐coated microspheres prepared in this work can be used as controlled release drug carriers with special needs.

Sensitive and precise visually guided drug delivery nanoplatform with dual activation of pH and light

Controlled-release drug carriers in cancer therapy are the most ideal way to reduce toxicity and improve drug efficacy. Since light stimulation is precise and operable, most multi-stimulation response carriers utilize phototherapy to enhance release efficiency. However, phototoxicity severely limits the application of phototherapy. Herein, we designed and synthesized a Cou-ONB lipid with sensitive fluorescence feedback and multi-stimulus response. COBL liposomes prepared from Cou-ONB lipids will passively aggregate at the tumor and guide phototherapy by fluorescence. More importantly, it can reflect the drug release effect in vivo through its own sensitive fluorescence changes, further enabling precise phototherapy and reducing phototoxicity. In this paper, the multi-stimulus superimposed response and precise fluorescence-guided performance of COBL liposomes were investigated at the molecular, liposome, cellular, and animal levels. Finally, tumor treatment experiments showed that the d-COBL-UV group had the best tumor suppression effect (5.3-fold). This paper highlights a real-time fluorescence-guided multi-stimulus superposition strategy and provides a design idea to precisely implement exogenous stimuli by displaying the degree of drug release, aiming to achieve less toxic and more efficient cancer therapy through timely and precise multi-stimulation. Statement of significanceMulti-stimulus responsive drug carriers have been extensively developed in the last decade. Visual guidance is an important tool to achieve precision medicine and precise control of drug release. However, the available visualization materials are more aimed at directing stimulation at the optimal moment. There is little discussion on when to stop exogenous stimulation and how to minimize the damage of stimulation to the patient. Here, we provide a Cou-ONB lipid that not only responds to multiple stimuli, but also provides sensitive feedback on its own dissociation with a fluorescent signal so that physicians can adjust exogenous stimuli in a timely manner. This paper provides insights to facilitate precision drug delivery systems, providing viable design ideas for precise, efficient, and less toxic cancer therapies.

Preparation and Sustained-Release Performance of PLGA Microcapsule Carrier System.

Microcapsules have been widely studied owing to their biocompatibility and potential for application in various areas, particularly drug delivery. However, the size of microcapsules is difficult to control, and the size distribution is very broad via various encapsulation techniques. Therefore, it is necessary to obtain microcapsules with uniform and tailored size for the construction of controlled-release drug carriers. In this study, emulsification and solvent evaporation methods were used to prepare a variety of ovalbumin-loaded poly (lactic-co-glycolic acid) (PLGA) microcapsules to determine the optimal preparation conditions. The particle size of the PLGA microcapsules prepared using the optimum conditions was approximately 200 nm, which showed good dispersibility with an ovalbumin encapsulation rate of more than 60%. In addition, porous microcapsules with different pore sizes were prepared by adding a varying amount of porogen bovine serum albumin (BSA) to the internal water phase. The release curve showed that the rate of protein release from the microcapsules could be controlled by adjusting the pore size. These findings demonstrated that we could tailor the morphology and structure of microcapsules by regulating the preparation conditions, thus controlling the encapsulation efficiency and the release performance of the microcapsule carrier system. We envision that this controlled-release novel microcapsule carrier system shows great potential for biomedical applications.

Preparation and characterization of sodium alginate/phosphate-stabilized amorphous calcium carbonate nanocarriers and their application in the release of curcumin

Phosphate-stabilized amorphous calcium carbonate (ACCP) has excellent biocompatibility, bioactivity, and biodegradability, and can be easily synthesized and stored. However, unmodified ACCP, as a controlled drug release carrier, decomposes rapidly in an acidic environment and highly depends on the system’s pH value, which can not meet the need for long-term release of active substances, thus limiting its application scope. To realize the specific pH responsiveness of ACCP nanoparticles, we designed and synthesized monodisperse sodium alginate/ACCP (Alginate/ACCP) composite nanoparticles in this paper. After ultrasonic treatment, nanoparticles with an average particle size less than 200 nm could form stable water dispersion that could be dispersed for up to 10 d. Based on the specific pH sensitivity of sodium alginate, the drug-controlled release performance of composite nanoparticles and the therapeutic effect of drug-loaded nanoparticles on A549 cancer cells were studied. The results indicated that under the same pH condition, the curcumin (Cur) release rate of composite nanoparticles gradually decreased with sodium alginate addition. When the dosage of sodium alginate was 1.0 mg ml−1, the cumulative drug release rate of nanoparticles in 40 h was only about 35%. Besides, the drug-loaded nanoparticles showed the excellent killing ability of cancer cells, and the survival rate of cancer cells decreased in a concentration-dependent manner. Therefore, through reasonable optimization design, we can synthesize composite nanoparticles with excellent sustained-release properties to provide a new strategy for cancer cells’ long-term treatment.

Formulation and Evaluation of Topical Proniosomal Gel of Ciclopirox for Antifungal Therapy

Objectives: The objective of existent effort was topical proniosomal gel formulation and evaluation from the proniosomes of Ciclopirox to improve poor skin penetration and residence of the topical antifungal drugs. Methods: The co-acervation phase separation method was used to prepare proniosomes by using combination of different grades of non-ionic surfactant, cholestrol and lecithin. Characterized for pH, encapsulation efficiency, Particle size, in vitro drug permeation. Selected batches were converted into topical proniosomal gel and evaluated for ex vivo permeation. Then best fitted formulation batch C5CF8 were differentiate with marketed preparation for ex vivo drug release and anti-fungal activity. Results: Proniosomal gel pH be there 5.61± 0.25 to 7.31± 0.06 and encapsulation efficiency 82.40 to 92.20% and particle size 3.20 ± 0.15 to 6.45 ± 0.20. In vitro drug release is in between 37.65 to 57.04 %. Among the formulations CF1, CF2, CF3, CF4 and CF5 were developed into carbopol topical gel as C1CF2, C2CF32, C3CF5, C4CF6 and C5CF8 and evaluated for ex vivo drug permeation. Among these optimized formulation C5CF8 showed drug permeation 59.39 ± 0.10 % at 12 hr. with a flux value of 5.24μg/ cm2/hr., permeability coefficient of 0.262 cm2/hr. and higher correlation coefficient R2 0.9949 for zero order drug release and hence follows zero order release kinetics. The C5F8 showed prolonged drug release and zone of inhibition value higher for carbopol gel as compared to marketed preparation Conclusion: Developed carbopol topical gel had potential to act as controlled release drug carrier which prolonged the drug release for number of hours.

Nanoscience and quantum science-led biocidal and antiviral strategies.

The severe acute respiratory syndrome coronavirus (SARS-CoV-2) caused the COVID-19 pandemic. According to the World Health Organization, this pandemic continues to be a serious threat to public health due to the worldwide spread of variants and their higher rate of transmissibility. A range of measures are necessary to slow the pandemic and save lives, which include constant evaluation and the careful adjustment of public-health responses augmented by medical treatments, vaccines and protective gear. It is hypothesized that nanostructured particulates underpinned by nanoscience and quantum science yield high-performing antiviral strategies, which can be applied in preventive, diagnostic, and therapeutic applications such as face masks, respirators, COVID test kits, vaccines, and drugs. This review is aimed at providing comprehensive and cohesive perspectives on various nanostructures that are suited to intensifying and amplifying the effectiveness of antiviral strategies. Growing scientific literature over the past eighteen months indicates that quantum dots, iron oxide, silicon oxide, polymeric and metallic nanoparticles have been employed in COVID-19 diagnostic assays, vaccines, and personal protective equipment (PPE). Quantum dots have displayed their suitability as more sensitive imaging probes in diagnostics and prognostics, and as controlled drug-release carriers that target the virus. Nanoscience and quantum science have assisted the design of advanced vaccine delivery since nanostructured materials are suited for antigen delivery, as mimics of viral structures and as adjuvants. Furthermore, the quantum science- and nanoscience-supported tailored functionalization of nanostructured materials offers insight and pathways to deal with future pandemics. This review seeks to illustrate several examples, and to explain the underpinning quantum science and nanoscience phenomena, which include wave functions, electrostatic interactions, van der Waals forces, thermal and electrodynamic fluctuations, dispersion forces, local field-enhancement effects, and the generation of reactive oxygen species (ROS). This review discusses how nanostructured materials are helpful in the detection, prevention, and treatment of the SARS-CoV-2 infection, other known viral infection diseases, and future pandemics.

Temperature and Photo Dual‐Stimuli Responsive Block Copolymer Self‐Assembly Micelles for Cellular Controlled Drug Release

To well adapt to the complicated physiological environments, it is necessary to engineer dual- and/or multi-stimuli responsive drug carriers for more effective drug release. For this, a novel temperature responsive lateral chain photosensitive block copolymer, poly[(N-isopropylacrylamide-co-N,N-dimethylacrylamide) -block-propyleneacylalkyl-4-azobenzoate] (P(NIPAM-co-DMAA)-b-PAzoHPA), is synthesized by atom transfer radical polymerization. The structure is characterized by 1 H nuclear magnetic resonance spectrometry and laser light scattering gel chromatography system. The self-assembly behavior, morphology, and sizes of micelles are investigated by fluorescence spectroscopy, transmission electron microscope, and laser particle analyzer. Dual responsiveness to light and temperature is explored by ultraviolet-visible absorption spectroscopy. The results show that the copolymer micelles take on apparent light and temperature dual responsiveness, and its lower critical solution temperature (LCST) is above 37 °C, and changes with the trans-/cis- isomerization of azobenzene structure under UV irradiation. The blank copolymers are nontoxic, whereas the paclitaxel (PTX)-loaded counterparts possessed comparable anticancer activities to free PTX, with entrapment efficiency of 83.7%. The PTX release from the PTX-loaded micelles can be mediated by changing temperature and/or light stimuli. The developed block copolymers can potentially be used for cancer therapy as drug controlled release carriers.

Fabrication of ultrafast temperature‐responsive nanofibrous hydrogel with superelasticity and its 'on–off' switchable drug releasing capacity

AbstractThe temperature‐responsive bulky hydrogel with fast response rate and satisfactory mechanical property has fascinating application potential in many aspects, such as the implantable macroscale controlled drug release carrier for post‐surgical therapy; however, creating such a smart hydrogel was proven extremely challenging. Here a novel type of temperature‐responsive bulky hydrogel with ultrafast response rate and super compressible elasticity was fabricated by the fibrous freeze‐shaping technique using shortened temperature‐responsive polymer based electrospun hollow nanofibers as building blocks, followed by heat treatment for endowing the hydrogel with high stability in water. Because the hydrogel has hierarchical porous structure and its constituent nanofibers have hollow structure, which are beneficial to diffusion of its embodied water during temperature‐induced volume phase transition, its temperature‐response time is less than 30 s. In addition, the hierarchical porous structure benefits dissipation of the compression stress exerted on the hydrogel. Fluorescein isothiocyanate (FITC)‐dextran as a model biomacromolecular drug, was loaded into the shells of the hollow nanofibers during coaxial electrospinning, and the ultimately obtained nanofibrous hydrogel can release its loaded FITC‐dextran in a 'on–off' switchable fashion in response to temperature alternation between 15 and 47°C. Cell cytotoxicity test results demonstrate that the temperature‐responsive nanofibrous hydrogel is biocompatible.

Radiation development of gastroretentive amoxicillin trihydrate floating-alginate based beads for the treatment of helicobacter pylori

Development of controlled drug release carriers with gastroretentive ability is one of the most feasible approaches to improve the bioavailability and efficiency of medical treatment of Helicobacter pylori-induced peptic ulcers. Consequently, modification of alginate with N, N-dimethylamino ethyl methacrylate was occurred via graft copolymerization technique using γ-irradiation. (Alg-g-DMAEMA) copolymers were used to prepare Amoxicillin-Trihydrate floated hollow beads using calcium chloride as crosslinker and calcium carbonate as a gas-forming agent to induce floatability. Swelling behavior, floatability, and gastric retention time were investigated in simulated gastric fluid. Morphological features, drug encapsulation efficiency, and in vitro (AT) release were evaluated. Beads show internal hollow construction with bulk density ranged from 0.393 to 1.533 (g/cm3) and enhanced gastric residence time extended up to 24 h. Drug entrapment efficiency ranged between 63 to 97% with sustainable release behavior extending beyond 15 h depends on beads p (DMAEMA) content. The newly developed pH-sensitive floated (AT) loaded (Alg-g-DMAEMA) beads are promising for increasing gastric residence time with sustained (AT) release which improves its bioavailability for the effective treatment of H. pylori. The in-vitro study showed that (AT) loaded beads eradicate more than 95% of H. pylori after 10 h.

Nitrogen Doped Porous Reduced Graphene Oxide Hybrid as a Nanocarrier of Imatinib Anticancer Drug

Nowadays, the cancer is one of the world’s most devastating diseases. The researches shows carbon nanomaterials as carriers for selective and controlled drug release and therapeutic agents. In this work, we developed new polymeric carbon nanocarrier based on nitrogen doped porous reduced graphene oxide (N-prGO)-carboxymethyl cellulose (CMC) as nanocarrier (NG-CMC) to load anticancer drug, imatinib (IM). The FE-SEM images, cyclic voltammetry, and Raman and UV-Vis spectroscopy methods confirmed the loading of IM on the NG-CMC. The results showed efficient loading of IM, ~74% at pH 7.00, time 3 h and 1 : 1 ratio of IM to NG-CMC onto NG-CMC. The biopolymer presence of CMC onto surface of nanocarrier due to the presence of –OH and –COOH groups interacts by hydrogen binding and π–π stacking with IM and enhanced the loading process of IM. The ~58.4, ~23.7, and ~16.2% of IM could be released from the NG- CMC upon the pH 4.00, 7.00, and 9.00, respectively, after 20 h. Thus, the development of present nanocarrier because of its unique physicochemical properties and high surface area is an ideal candidate for nanoscale assembly and able to deliver anticancer agents into cells.

Synthesis of the Core-Shell Structure Materials as the Controlled-Release Drug Carrier

Synthesis of the Core-Shell Structure Materials as the Controlled-Release Drug Carrier

Formulation and Evaluation of Proniosomal Topical Antifungal Gel of Miconazole Nitrate

Proniosomal gel formulations of miconazole nitrate (MCZ) were prepared by using combinations of different grades of (non-ionic surfactant) span, cholesterol, and lecithin by coacervation phase separation method. Developed 10 proniosomal gel formulations were characterized for particle size, shape, % entrapment efficiency, drug content, in vitro drug permeation, scanning electron microscopy (SEM), DSC, stability study. The fourier transform infrared spectroscopy (FTIR) studies confirmed the compatibility of the drug with excipients. The results showed that all the formulations were pale yellow to pale brown in color, pH was is in the range of 5.60 to 7.20, and encapsulation efficiency was found is in the range of 83 to 91.25% and particle size in between 5.81 ± 0.2 to 07.52 ± 0.07. Among the ten formulations MF2, MF3, MF5, MF6, and MF8 showed maximum drug release in a controlled manner at 12 hours of study and developed into carbopol proniosomal topical gel and evaluated for ex-vivo drug permeation. Formulationoptimized formulation C5MF8 showed higher drug permeation 74.19 ± 0.16% at 12 hr. with a flux valueof 6.829 ± 0.12 μg/cm2 /hr. The permeability coefficient of 0.341 ±0.08 cm2 /hrs., higher correlation coefficient R2 0.9944 for zero-order drug release kinetic model, and follows zero-order release kinetics. Among the 5 formulations, optimized carbopol proniosomal topical gel formulation C5MF8 drug release and in-vitro antifungal activity was compared with marketed formulation cream.C5MF8 showed sustain drug release and zone of inhibition value was very near to marketed preparation. Hence it was concluded that developed carbopol proniosomal topical gel had the potential to act as a controlled release drug carrier,which sustains the drug release for many hours and exhibit good antifungal activity

Dual Stimuli-Responsive Supramolecular Self-Assemblies Based on the Host-Guest Interaction between β-Cyclodextrin and Azobenzene for Cellular Drug Release.

Health has always been a hot topic of concern, whereas cancer is one of the largest security risks to human health. Although the existing drug delivery systems (DDSs) have been extensively reported and commercially applied, there are still some issues that have yet to be well-resolved, including the toxicity, side-effects, and targeted therapy efficiency of drugs. Consequently, it is still necessary to develop a novel, highly efficient, controlled and targeted DDS for cancer therapy. For this, a supramolecular polymer, β-CD-g-PDMAEMA@Azo-PCL, was designed and developed through the host-guest inclusion complexation interactions between a host polymer, β-cyclodextrin-graft-poly(2-(dimethylamino)ethyl methacrylate) (β-CD-g-PDMAEMA), and a guest polymer, azobenzene modified poly(ε-caprolactone) (Azo-PCL), and was characterized by various analysis techniques. The supramolecular assembly was examined in various pH environments and/or under UV-vis irradiation, showing the formation of supramolecular assemblies from regular spherical shapes to irregular aggregates with various hydrodynamic diameters. The 2D NOESY NMR studies showed the formation of inclusion complexation between Azo-PCL and β-CD-g-PDMAEMA and between β-CD and the side groups of PDMAEMA. The supramolecular assemblies could encapsulate doxorubicin to form spherical core-shell drug-carrying micelles with an entrapment efficiency of 66.1%. The effects of external environment stimuli on the in vitro drug release were investigated, showing light- and pH-modulated drug release properties. The cytotoxicity assessment indicated that the blank supramolecular micelles were nontoxic, whereas the drug-loaded micelles exhibited comparable or even superior anticancer activity to the anticancer activity of free DOX and inhibition of cancer cell proliferation. Therefore, the developed supramolecular assemblies can potentially be used as drug-controlled release carriers.