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"Polymeric drug delivery system"
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Enhancement of lemongrass essential oil physicochemical properties and antibacterial activity by encapsulation in zein-caseinate nanocomposite
by
Baghdadi, Hoda H.
,
El-Hosseiny, Lobna S.
,
El-Shenawy, Moustafa A.
in
631/326
,
639/925
,
Alkaline phosphatase
2024
Essential oils (EOs) represent a pivotal source for developing potent antimicrobial drugs. However, EOs have seldom found their way to the pharmaceutical market due to their instability and low bioavailability. Nanoencapsulation is an auspicious strategy that may circumvent these limitations. In the current study, lemongrass essential oil (LGO) was encapsulated in zein-sodium caseinate nanoparticles (Z-NaCAS NPs). The fabricated nanocomposite was characterized using dynamic light scattering, Fourier-transform infrared spectroscopy, differential scanning calorimetry, and transmission electron microscopy. The antimicrobial activity of LGO loaded NPs was assessed in comparison to free LGO against
Staphylococcus epidermidis, Enterococcus faecalis, Escherichia coli,
and
Klebsiella pneumoniae
. Furthermore, their antibacterial mechanism was examined by alkaline phosphatase, lactate dehydrogenase, bacterial DNA and protein assays, and scanning electron microscopy. Results confirmed the successful encapsulation of LGO with particle size of 243 nm, zeta potential of – 32 mV, and encapsulation efficiency of 84.7%. Additionally, the encapsulated LGO showed an enhanced thermal stability and a sustained release pattern. Furthermore, LGO loaded NPs exhibited substantial antibacterial activity, with a significant 2 to 4 fold increase in cell wall permeability and intracellular enzymes leakage versus free LGO. Accordingly, nanoencapsulation in Z-NaCAS NPs improved LGO physicochemical and antimicrobial properties, expanding their scope of pharmaceutical applications.
Journal Article
Linker-Free Hyaluronic Acid-Dexamethasone Conjugates: pH-Responsive Nanocarriers for Targeted Anti-Inflammatory Therapy
2025
The covalent conjugation of pharmaceutical compounds to polymeric carriers represents an effective strategy for enhancing drug properties, including improved bioavailability, targeted delivery, and sustained release, while reducing systemic toxicity and adverse effects. By exploiting the physicochemical characteristics of biopolymers—particularly molecular charge and weight—we engineered a polymeric platform for glucocorticoid delivery with precisely controlled parameters including particle size, surface charge, targeting capability, and release kinetics. This study reports a linker-free synthesis of hyaluronic acid-dexamethasone (HA-DEX) conjugates through Steglich esterification, catalyzed by 4-dimethylaminopyridine (DMAP), which facilitates the acylation of sterically hindered alcohols. The reaction specifically couples carboxyl groups of hyaluronic acid with the C21 hydroxyl group of dexamethasone. Incorporation of hydrophobic dexamethasone moieties induced self-assembly into nanoparticles featuring a hydrophobic core and negatively charged hydrophilic shell (−20 to −25 mV ζ-potential). In vitro characterization revealed pH-dependent release profiles, with 80–90% dexamethasone liberated in mildly acidic phosphate buffer (pH 5.2) versus 50–60% in phosphate-buffered saline (pH 7.4) over 35 days, demonstrating both sustained release and inflammation-responsive behavior. The conjugates exhibited potent anti-inflammatory activity in a human tumor necrosis factor-α (TNFα)-induced inflammation model. These findings position HA-DEX conjugates as promising candidates for targeted glucocorticoid delivery to specific anatomical sites including ocular, articular, and tympanic tissues, where their combination of CD44-targeting capability, enhanced permeability and retention effects, and stimulus-responsive release can optimize therapeutic outcomes while minimizing off-target effects.
Journal Article
A new composite nanofibrous biomaterial development for drug delivery applications
by
Cengiz Callioglu, Funda
,
Kesici Güler, Hülya
in
Bioavailability
,
Biomedical materials
,
biopolymers, biocomposites
2023
This study aims to produce drug delivery systems using ultrasonic spray pyrolysis (USP) and electrospinning methods. For this purpose, the study was carried out in two steps. In the first step, polyvinylpyrrolidone (PVP)/gelatin (GEL) based nanofibers were produced by the electrospinning method. The nanofibers were coated with azithromycin (AZI) in the second step using the USP method. Finally, characterization studies such as morphological, chemical, and thermal were carried out, and drug release behaviors were analyzed. The findings show that nanofibers are noticeably fine, smooth, and uniform. Although burst release was observed for the first time because the drug molecules were located on the nanofibrous surface, the release time was increased from 30 min to 48 h by obtaining sandwich structures. The results showed that the USP method could be used to produce new drug delivery systems with the electrospinning method.
Journal Article
Co-Encapsulation and Co-Delivery of Peptide Drugs via Polymeric Nanoparticles
by
Feng, Teng
,
Zhang, Qian
,
Chan, Ho Yin Edwin
in
Biocompatibility
,
Cytotoxicity
,
Dehydrogenases
2019
Combination therapy is a promising form of treatment. In particular, co-treatment of P3 and QBP1 has been shown to enhance therapeutic effect in vivo in treating polyglutamine diseases. These peptide drugs, however, face challenges in clinical administration due to poor stability, inability to reach intracellular targets, and lack of method to co-deliver both drugs. Here we demonstrate two methods of co-encapsulating the peptide drugs via polymer poly(ethylene glycol)-block-polycaprolactone (PEG-b-PCL) based nanoparticles. Nanoparticles made by double emulsion were 100–200 nm in diameter, with drug encapsulation efficiency of around 30%. Nanoparticles made by nanoprecipitation with lipid 1-palmitoyl-2-oleoyl-sn-glycero-3-phospho-(1′-rac-glycerol) (POPG) were around 250–300 nm in diameter, with encapsulation efficiency of 85–100%. Particles made with both formulations showed cellular uptake when decorated with a mixture of peptide ligands that facilitate endocytosis. In vitro assay showed that nanoparticles could deliver bioactive peptides and encapsulation by double emulsion were found to be more effective in rescuing cells from polyglutamine-induced toxicity.
Journal Article
Recent Advances in Polymeric Drug Delivery Systems for Peripheral Nerve Regeneration
by
Redolfi Riva, Eugenio
,
Bianchini, Marta
,
Micera, Silvestro
in
Biocompatibility
,
Biodegradable materials
,
Biomedical materials
2023
When a traumatic event causes complete denervation, muscle functional recovery is highly compromised. A possible solution to this issue is the implantation of a biodegradable polymeric tubular scaffold, providing a biomimetic environment to support the nerve regeneration process. However, in the case of consistent peripheral nerve damage, the regeneration capabilities are poor. Hence, a crucial challenge in this field is the development of biodegradable micro- nanostructured polymeric carriers for controlled and sustained release of molecules to enhance nerve regeneration. The aim of these systems is to favor the cellular processes that support nerve regeneration to increase the functional recovery outcome. Drug delivery systems (DDSs) are interesting solutions in the nerve regeneration framework, due to the possibility of specifically targeting the active principle within the site of interest, maximizing its therapeutical efficacy. The scope of this review is to highlight the recent advances regarding the study of biodegradable polymeric DDS for nerve regeneration and to discuss their potential to enhance regenerative performance in those clinical scenarios characterized by severe nerve damage.
Journal Article
Preformulation Study of Controlled-Release Galantamine Matrix Tablets Containing Polyethylene Oxide, Hydroxypropyl Methylcellulose, and Ethylcellulose
by
González-Barrios, Andrés F.
,
Osorio, Edison H.
,
Villegas-Torres, María Francisca
in
Cellulose
,
compaction behavior
,
controlled-release matrix tablets
2025
Background/Objectives: The rational design of modified-release matrix tablets requires a thorough understanding of granulometric analysis, compaction behavior, and drug release profile. In this study, we evaluated the physicochemical, granulometric, and mechanical properties of hydroxypropyl methylcellulose, polyethylene oxide, and ethylcellulose in galantamine matrix formulations. Methods: Spectroscopic (FTIR) and thermal (DSC) analyses demonstrated drug–polymer compatibility. We assessed flowability, cohesion, and aeration behavior through granulometric analysis and applied compressibility models (Kawakita, Heckel, Leuenberger) to characterize deformation mechanisms. Results: Hydroxypropyl methylcellulose showed superior compactability (Tmax = 4.61 MPa) and sustained drug release (85.4% at 12 h, DE% = 62.2%), while polyethylene oxide enabled gradual erosion and consistent delivery (88.7% at 12 h, DE% = 57.5%). In contrast, ethylcellulose exhibited high cohesiveness but poor matrix integrity, leading to premature drug release (76.6% at 1 h, DE% = 73.7%). Only hydroxypropyl methylcellulose and polyethylene oxide formulations met USP criteria. Conclusions: These results demonstrate that polymer selection critically influences powder behavior and matrix performance, underscoring the need for integrated granulometric and mechanical evaluation in the development of robust controlled-release systems.
Journal Article
Size and charge characterization of polymeric drug delivery systems by Taylor dispersion analysis and capillary electrophoresis
by
Meyrueix, Rémi
,
Cottet, Hervé
,
Chan, You Ping
in
Analytical Chemistry
,
Biochemistry
,
biopharmaceuticals
2013
In this work, Taylor dispersion analysis and capillary electrophoresis were used to characterize the size and charge of polymeric drug delivery nanogels based on polyglutamate chains grafted with hydrophobic groups of vitamin E. The hydrophobic vitamin E groups self-associate in water to form small hydrophobic nanodomains that can incorporate small drugs or therapeutic proteins. Taylor dispersion analysis is well suited to determine the weight average hydrodynamic radius of nanomaterials and to get information on the size polydispersity of polymeric samples. The effective charge was determined either from electrophoretic mobility and hydrodynamic radius using electrophoretic modeling (three different approaches were compared), or by indirect UV detection in capillary electrophoresis. The influence of vitamin E hydrophobicity on the polymer effective charge has been studied. The presence of vitamin E leads to a drastic decrease in polymer effective charge in comparison to non-modified polyglutamate. Finally, the electrophoretic behavior of polyglutamate backbone grafted with hydrophobic vitamin E (pGVE) nanogels according to the ionic strength was investigated using the recently proposed slope plot approach. It was deduced that the pGVE nanogels behave electrophoretically as polyelectrolytes which is in good agreement with the high water content of the nanogels.
Figure
Size and charge characterization of polyglutamate-based drug delivery systems by Taylor dispersion analysis, indirect UV detection and the 'Slope-plot' approach
Journal Article
Bioresorbable Nonwoven Patches as Taxane Delivery Systems for Prostate Cancer Treatment
by
Godzierz, Marcin
,
Hercog, Anna
,
Orchel, Arkadiusz
in
cabazitaxel
,
Cancer therapies
,
Care and treatment
2022
Prostate cancer is the second most common cancer in males. In the case of locally advanced prostate cancer radical prostatectomy is one of the first-line therapy. However, recurrence after resection of the tumor can appear. Drug-eluting bioresorbable implants acting locally in the area of the tumor or the resection margins, that reduce the risk of recurrence would be advantageous. Electrospinning offers many benefits in terms of local delivery so fiber-forming polyesters and polyestercarbonates which are suitable to be drug-loaded were used in the study to obtain CTX or DTX-loaded electrospun patches for local delivery. After a fast verification step, patches based on the blend of poly(glycolide-ε-caprolactone) and poly(lactide-glycolide) as well as patches obtained with poly(lactide-glycolide- ε-caprolactone) were chosen for long-term study. After three months, 60% of the drug was released from (PGCL/PLGA) + CTX and it was selected for final, anticancer activity analysis with the use of PC-3 and DU145 cells to establish its therapeutic potential. CTX-loaded patches reduced cell growth to 53% and 31% respectively, as compared to drug-free patches. Extracts from drug-free patches showed excellent biocompatibility with the PC-3 cell line. Cabazitaxel-loaded bioresorbable patches are a promising drug delivery system for prostate cancer therapy.
Journal Article
Prazosin-Conjugated Matrices Based on Biodegradable Polymers and α-Amino Acids—Synthesis, Characterization, and in Vitro Release Study
by
Oledzka, Ewa
,
Skrzypczak, Agata
,
Kolodziejski, Waclaw
in
Adrenergic alpha-1 Receptor Antagonists - chemical synthesis
,
Adrenergic alpha-1 Receptor Antagonists - chemistry
,
Aliivibrio fischeri - drug effects
2015
Novel and promising macromolecular conjugates of the α1-adrenergic blocker prazosin were directly synthesized by covalent incorporation of the drug to matrices composed of biodegradable polymers and α-amino acids for the development of a polymeric implantable drug delivery carrier. The cyto- and genotoxicity of the synthesized matrices were evaluated using a bacterial luminescence test, protozoan assay, and Salmonella typhimurium TA1535. A new urethane bond was formed between the hydroxyl end-groups of the synthesized polymer matrices and an amine group of prazosin, using 1,1′-carbonyldiimidazole (CDI) as a coupling agent. The structure of the polymeric conjugates was characterized by various spectroscopy techniques. A study of hydrogen nuclear magnetic resonance (1H-NMR) and differential scanning calorimetry (DSC) thermodiagrams indicated that the presence of prazosin pendant groups in the macromolecule structures increased the polymer’s rigidity alongside increasing glass transition temperature. It has been found that the kinetic release of prazosin from the obtained macromolecular conjugates, tested in vitro under different conditions, is strongly dependent on the physicochemical properties of polymeric matrices. Furthermore, the presence of a urethane bond in the macromolecular conjugates allowed for obtaining a relatively controlled release profile of the drug. The obtained results confirm that the pharmacokinetics of prazosin might be improved through the synthesis of polymeric conjugates containing biomedical polymers and α-amino acids in the macromolecule.
Journal Article
Engineering Polymer Systems for Improved Drug Delivery
2014,2013
Polymers have played a critical role in the rational design and application of drug delivery systems that increase the efficacy and reduce the toxicity of new and conventional therapeutics. Beginning with an introduction to the fundamentals of drug delivery, Engineering Polymer Systems for Improved Drug Delivery explores traditional drug delivery techniques as well as emerging advanced drug delivery techniques. By reviewing many types of polymeric drug delivery systems, and including key points, worked examples and homework problems, this book will serve as a guide to for specialists and non-specialists as well as a graduate level text for drug delivery courses.