5 research outputs found
Development of lutein nanocarrier and evaluation of its effect on retinal angiogenesis in the hyperglycaemic animal model.
No full textDiabetic retinopathy (DR) is a frequent microvascular complication of diabetes and a
major cause of vision loss globally. DR ranked as the fifth most common cause of preventable
blindness and the fifth most common cause of moderate to severe visual impairment. The low
bioavailability of the drugs at the target site imposed by the anatomic and physiologic barriers
within the eye requires long-term treatments with frequent injections that often compromise
patient’s compliance and increase the risk of developing more complications. In recent years,
much effort has been put towards developing new drug delivery platforms aiming to enhance
their permeation, prolong their retention time at the target site and provide a sustained release
profile with reduced toxicity and improved efficacy. Hence, the present study aimed to enhance
lutein bioavailability and bioefficacy by encapsulating it in a hybrid polymer-lipid-based
nanocarrier system. It is hypothesized that the “Lutein loaded nanocarrier system enhances the
solubility, stability bioavailability and bioefficacy of lutein and also helps in slow and controlled
release of lutein at the target site to modulate oxidative stress and inflammation in delaying or
preventing retinal angiogenesis through the restoration of angiogenic markers in STZ induced
diabetic rat”
Boosting Curcumin Bioavailability: Unveiling the Potential of Sodium Caseinate Nanoparticle Microneedle Patches
No full textCurcumin is a well-known anti-obesity compound with limited clinical application due to its poor bioavailability at the target
site. Hence, we hypothesized that the curcumin sodium caseinate nanoparticles (CNC) loaded in microneedle patches (MNPs)
may improve curcumin bioavailability. The CNC were prepared with a microemulsion technique using clove oil, sodium casein-
ate to form nanoparticles and PEG 400 as a stabilizer and exhibited smaller particle size (100–250 nm) and polydispersity index
(0.201) with higher zeta potential (−45 mV) and entrapment efficiency (90%–95%). The CNC improved solubility, bioaccessibility
(7.2 fold) and bioavailability (2.6 fold) compared to native curcumin. Further, the CNC-loaded MNPs were developed by the
micro-molding and displayed a slow and controlled release of curcumin with superior bioavailability in the plasma (200 ng/mL)
and adipose (435 ng/mL) tissue of C57BL6 mice. Overall, the study advocates the novel CNC-loaded MNPs as a potential cur-
cumin delivery tool for treating obesity
Lutein encapsulated oleic - linoleic acid nanoemulsion boosts oral bioavailability of the eye protective carotenoid lutein in rat model
No full textThere is great interest in emerging colloidal delivery systems to enhance the water solubility and oral
bioavailability of lutein, a hydrophobic carotenoid claimed to possess health benefits. The present study aimed to
design lutein-enriched nanoemulsions with improved physicochemical properties and achieve various health
benefits. The prepared lutein nanoemulsion was characterized and its bioavailability was examined in vitro
(simulated gastrointestinal digestion) and in vivo. The mean size, PDI and zeta potential of the lutein nano�emulsion were 110 ± 8 nm, 0.271 and 36 ± 2 mV, respectively. Furthermore, TEM examination revealed that the
particles are nanosized and spherical. Notably, the aqueous solubility of the nanoemulsion was 726-fold higher
than that of free lutein. The composite nanoemulsion also showed exceptionally higher (87.4 %) in vitro bio�accessibility than nonencapsulated or free lutein (15 %). The in vivo bioavailability of lutein nanoemulsion
(112.6 ng/mL) was much higher than that of nonencapsulated lutein (48.6 ng/mL) and mixed micelles (68.5 ng/
mL) and the tissue distribution pattern of lutein nanoemulsion showed higher lutein accumulation in the liver
(2.80 and 1.70 fold) and eye (1.91 and 1.48 fold) compared to free lutein and mixed micelle-fed groups. These
results suggested that oleic acid-linoleic acid composite nanoemulsions may be a promising delivery system for
lutein and may help enhance the solubility, oral bioavailability and bioefficacy of lutein and could be used as an
ingredient for the formulation of beverages or functional foods
Using a Bacterial Protein to Selectively Target Bacterial Biofilms: Treatment of S. epidermidis Biofilms with Targeted Photothermal Gold Nanoparticle
No full textBiofilm-related infections are associated with high mortality and morbidity combined with increased treatment costs. Traditional antibiotics are becoming less effective due to the emergence of drug-resistant bacterial strains. The need to treat biofilms on medical implants is particularly acute, and one persistent challenge is selectively directing nanoparticles to the biofilm site. Here, we present a protein-based functionalization strategy that targets the extracellular matrix of biofilms. The engineered protein combines the Staphylococcus epidermidis autolysin R2ab domain with a gold-binding GB3 domain, directing nanoparticles specifically to bacterial cell wall components (lipoteichoic acid and wall teichoic acid) that are absent in mammalian tissues. This fusion protein is applied to a gold nanoparticle (AuNP) core, along with elastin-like polypeptides (ELPs), which generate a robust photothermal response. The engineered particles exhibit exceptional biocompatibility, including low protein corona formation, minimal macrophage uptake, and hemocompatibility, while maintaining selective biofilm targeting. The photothermal conversion can be modulated by changing the ELP transition temperature, and the functionalized AuNPs strongly interact with biofilms under static and flow conditions without significantly binding to serum-coated surfaces. Near-infrared laser irradiation resulted in a 10,000-fold improvement in killing efficiency compared to untreated controls (p \u3c 0.0001). The targeting strategy utilized here represents a versatile approach to targeting drug-resistant infections and could be readily expanded to other bacterial pathogens and anti-biofilm nanoparticle platforms
Postpolymerization Modification of Poly(2-vinyl-4,4-dimethyl azlactone) as a Versatile Strategy for Drug Conjugation and Stimuli-Responsive Release
No full textPostpolymerization modification of highly defined “scaffold”
polymers is a promising approach for overcoming the existing limitations
of controlled radical polymerization such as batch-to-batch inconsistencies,
accessibility to different monomers, and compatibility with harsh
synthesis conditions. Using multiple physicochemical characterization
techniques, we demonstrate that poly(2-vinyl-4,4-dimethyl azlactone)
(PVDMA) scaffolds can be efficiently modified with a coumarin derivative,
doxorubicin, and camptothecin small molecule drugs. Subsequently,
we show that coumarin-modified PVDMA has a high cellular biocompatibility
and that coumarin derivatives are liberated from the polymer in the
intracellular environment for cytosolic accumulation. In addition,
we report the pharmacokinetics, biodistribution, and antitumor efficacy
of a PVDMA-based polymer for the first time, demonstrating unique
accumulation patterns based on the administration route (i.e., intravenous
vs oral), efficient tumor uptake, and tumor growth inhibition in 4T1
orthotopic triple negative breast cancer (TNBC) xenografts. This work
establishes the utility of PVDMA as a versatile chemical platform
for producing polymer-drug conjugates with a tunable, stimuli-responsive
delivery
