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1.
Food Chem ; 458: 140295, 2024 Jul 01.
Article in English | MEDLINE | ID: mdl-38981397

ABSTRACT

Curcumin (Cur) as a natural food additive and photosensitizer has been widely applied on photodynamic sterilization and preservation for food, but the poor aqueous solubility and light stability restrict its extensive application. In this study, we report a Cur nanocapsules (Cur-CDs) made by carbon dots (CDs). Attributing to the hydrogen bonds formed between Cur and CDs, Cur-CDs exhibits excellent Cur aqueous solubility each to 9286.98 ng/mL (enhanced by 246.27 times) and light stability (enhanced by 1.51 times). The photogenerated electron transmission from Cur to CDs in addition resulted in >1.23 and 1.60 times generation of •O2- and •OH, compared to that of bare Cur. Accordingly, 5.73 × 103 CFU L. monocytogenes, and 5.43 × 103 CFU S. aureus were killed by 0.06 mg/mL Cur-CDs within 20 mins of blue light, showing the promising potential in the development and application of safe and environmentally friendly non-thermal sterilization technology based on Cur-CDs.

2.
Heliyon ; 10(12): e32808, 2024 Jun 30.
Article in English | MEDLINE | ID: mdl-38975186

ABSTRACT

For decades, animal models have been the standard approach in drug research and development, as they are required by regulations in the transition from preclinical to clinical trials. However, there is growing ethical and scientific concern regarding these trials, as 80 % of the therapeutic potential observed in pre-clinical studies are often unable to be replicated, despite demonstrating efficacy and safety. In response to this, Tissue Engineering has emerged as a promising alternative that enables the treatment of various diseases through the production of biological models for advanced biological assays or through the direct development of tissue repairs or replacements. One of the promising applications of Tissue Engineering is the development of three-dimensional (3D) models for in vitro tests, replacing the need for in vivo animal models. In this study, 3D skin equivalents (TSE) were produced and used as an in vitro model to test photobiostimulation using curcumin-loaded nanocapsules. Photodynamic biostimulation therapy uses photodynamic processes to generate small amounts of reactive oxygen species (ROS), which can activate important biological effects such as cell differentiation, modulation of inflammatory processes and contribution to cell regeneration. The PLGA nanocapsules (NC) used in the study were synthesized through a preformed polymer deposition method, exhibiting particle size <200 nm, Zeta potential >|30| and polydispersity index between 0.5 and 0.3. Atomic force microscopy analyzes confirmed that the particle size was <200 nm, with a spherical morphology and a predominantly smooth and uniform surface. The NC biocompatibility assay did not demonstrate cytotoxicity for the concentrations tested (2.5-25 µg mL-1).The in vitro release assay showed a slow and sustained release characteristic of the nanocapsules, and cellular uptake assays indicated a significant increase in cellular internalization of the curcumin-loaded nanostructure. Monolayer photobiostimulation studies revealed an increase in cell viability of the HDFn cell line (viability 134 %-228 %) for all LED fluences employed at λ = 450 nm (150, 300, and 450 mJ cm-2). Additionally, the scratch assays, monitoring in vitro scar injury, demonstrated more effective effects on cell proliferation with the fluence of 300 mJ cm-2. Staining of TSE with hematoxylin and eosin showed the presence of cells with different morphologies, confirming the presence of fibroblasts and keratinocytes. Immunohistochemistry using KI-67 revealed the presence of proliferating cells in TSE after irradiation with LED λ = 450 nm (150, 300, and 450 mJ cm-2).

3.
Adv Sci (Weinh) ; : e2403668, 2024 Jul 08.
Article in English | MEDLINE | ID: mdl-38973298

ABSTRACT

Nanocapsules enable multicomponent encapsulation of therapeutic cargoes with high encapsulation content and efficiency, which is vital for cancer immunotherapy. In the past, chemical crosslinking is used to synthesize nanocapsules, which can impede the regulatory approval process. Therefore, a new class of protein nanocapsules is developed by eliminating the need for chemical crosslinking by utilizing protein denaturation through a process that is referred to as "baking at the droplet interface". Such protein nanocapsules with antigens incorporated in the shell and a combination of encapsulated drugs showed an enhancement in the immune response of cells.

4.
Indian J Microbiol ; 64(2): 429-444, 2024 Jun.
Article in English | MEDLINE | ID: mdl-39010996

ABSTRACT

Lipids have tremendously transformed the biomedical field, especially in the last few decades. Nanosystems, especially Lipid nanocapsules (LNCs), have emerged as the most demanding nanovehicle systems for delivering drugs, genes, and other diagnostic agents. Unique attributes and characteristic features such as higher encapsulation efficiency, stealth effect, ability to solubilize a wide range of drugs, capability to inhibit P-gp efflux pumps, and higher stability play a vital role in engaging this nanosystem. LNCs are a lipid-based nano-drug delivery method that combines the most significant traits of liposomes with polymeric nanoparticles. Structurally, LNCs have an oily core consisting of medium and long triglycerides and an aqueous phase encased in an amphiphilic shell. This manuscript crosstalks LNCs for various biomedical applications. A detailed elaboration of the structural composition, methods of preparation, and quality control aspects has also been attained, with particular emphasis on application approaches, ongoing challenges, and their possible resolution. The manuscript also expounds the preclinical data and discusses the patents atlas of LNCs to assist biomedical scientists working in this area and foster additional research. Supplementary Information: The online version contains supplementary material available at 10.1007/s12088-024-01298-3.

5.
Int J Pharm ; 661: 124458, 2024 Jul 10.
Article in English | MEDLINE | ID: mdl-38996823

ABSTRACT

Leukemia, particularly acute myeloid leukemia (AML) is considered a serious health condition with high prevalence among adults. Accordingly, finding new therapeutic modalities for AML is urgently needed. This study aimed to develop a biocompatible nanoformulation for effective oral delivery of the phytomedicine; baicalin (BAC) for AML treatment. Lipid nanocapsules (LNCs) based on bioactive natural components; rhamnolipids (RL) as a biosurfactant and the essential oil linalool (LIN), were prepared using a simple phase-inversion method. The elaborated BAC-LNCs displayed 61.1 nm diameter and 0.2 PDI. Entrapment efficiency exceeded 98 % with slow drug release and high storage-stability over 3 months. Moreover, BAC-LNCs enhanced BAC oral bioavailability by 2.3-fold compared to BAC suspension in rats with higher half-life and mean residence-time. In vitro anticancer studies confirmed the prominent cytotoxicity of BAC-LNCs on the human leukemia monocytes (THP-1). BAC-LNCs exerted higher cellular association, apoptotic capability and antiproliferative activity with DNA synthesis-phase arrest. Finally, a mechanistic study performed through evaluation of various tumor biomarkers revealed that BAC-LNCs downregulated the angiogenic marker, vascular endothelial growth-factor (VEGF) and the anti-apoptotic marker (BCl-2) and upregulated the apoptotic markers (Caspase-3 and BAX). The improved efficacy of BAC bioactive-LNCs substantially recommends their pharmacotherapeutic potential as a promising nanoplatform for AML treatment.

6.
Int J Mol Sci ; 25(11)2024 May 28.
Article in English | MEDLINE | ID: mdl-38892083

ABSTRACT

Oil-core nanocapsules (NCs, also known as nanoemulsions) are of great interest due to their application as efficient carriers of various lipophilic bioactives, such as drugs. Here, we reported for the first time the preparation and characterization of NCs consisting of chondroitin sulfate (CS)-based shells and liquid oil cores. For this purpose, two amphiphilic CS derivatives (AmCSs) were obtained by grafting the polysaccharide chain with octadecyl or oleyl groups. AmCS-based NCs were prepared by an ultrasound-assisted emulsification of an oil phase consisting of a mixture of triglyceride oil and vitamin E in a dispersion of AmCSs. Dynamic light scattering and cryo-transmission electron microscopy showed that the as-prepared core-shell NCs have typical diameters in the range of 30-250 nm and spherical morphology. Since CS is a strong polyanion, these particles have a very low surface potential, which promotes their stabilization. The cytotoxicity of the CS derivatives and CS-based NCs and their impact on cell proliferation were analyzed using human keratinocytes (HaCaTs) and primary human skin fibroblasts (HSFs). In vitro studies showed that AmCSs dispersed in an aqueous medium, exhibiting mild cytotoxicity against HaCaTs, while for HSFs, the harmful effect was observed only for the CS derivative with octadecyl side groups. However, the nanocapsules coated with AmCSs, especially those filled with vitamin E, show high biocompatibility with human skin cells. Due to their stability under physiological conditions, the high encapsulation efficiency of their hydrophobic compounds, and biocompatibility, AmCS-based NCs are promising carriers for the topical delivery of lipophilic bioactive compounds.


Subject(s)
Chondroitin Sulfates , Drug Carriers , Nanocapsules , Nanocapsules/chemistry , Humans , Chondroitin Sulfates/chemistry , Drug Carriers/chemistry , Dietary Supplements , Fibroblasts/drug effects , Cell Proliferation/drug effects , Keratinocytes/drug effects , Emulsions/chemistry , Particle Size , Vitamin E/chemistry , Cell Survival/drug effects , Cell Line , HaCaT Cells
7.
Int J Biol Macromol ; 273(Pt 2): 132972, 2024 Jul.
Article in English | MEDLINE | ID: mdl-38876241

ABSTRACT

The use of essential oils as natural antioxidant, antimicrobial and insect repellent agent was limited by the loss of bioactive components especially volatile compounds. This study aimed to improve biological properties of curry leaf essential oil (CLEO) by producing nanometer sized particles through two different synthesis techniques; nanoencapsulation and nanoprecipitation. The methods produced different nanostructures; nanocapsules and nanospheres distinguished by the morphological structure (TEM analysis). Successful loading of CLEO into chitosan nanocarrier was proven by FTIR spectra. Zeta potential values for both nanostructures were more than +30 mV implying their stability against aggregation. CLEO loaded nanocapsules exhibited highest antibacterial properties against Gram-positive bacteria compared to nanospheres. Meanwhile, CLEO loaded nanospheres recorded up until 90.44 % DPPH radical scavenging properties, higher compared to nanocapsules. Both nanostructures demonstrated further improvement in antioxidant and antibacterial activities with the incorporation of higher chitosan concentration. In vitro release analysis indicated that CLEO undergo two-stage discharge mechanism where fast discharge occurred up until 12 h followed by sustained released afterwards. The two synthesis methods applied synergistically with greater chitosan concentration successfully produced nanostructures with >60 % encapsulation efficiency (EE). This concluded that both techniques were reliable to protect the bioactive constituents of CLEO for further used.


Subject(s)
Anti-Bacterial Agents , Antioxidants , Chitosan , Drug Liberation , Nanoparticles , Oils, Volatile , Plant Leaves , Chitosan/chemistry , Chitosan/pharmacology , Oils, Volatile/chemistry , Oils, Volatile/pharmacology , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/chemistry , Plant Leaves/chemistry , Antioxidants/chemistry , Antioxidants/pharmacology , Nanoparticles/chemistry , Chemical Phenomena , Microbial Sensitivity Tests , Drug Carriers/chemistry , Particle Size , Nanocapsules/chemistry
8.
Int J Pharm ; 660: 124304, 2024 Jul 20.
Article in English | MEDLINE | ID: mdl-38848799

ABSTRACT

Depression is one of the most common psychiatric disorders. Nanotechnology has emerged to optimize the pharmacological response. Therefore, the aim of this work was to develop and characterize liposomes and nanocapsules containing paroxetine hydrochloride and evaluate their antidepressant-like effect using the open field and tail suspension tests in mice. Liposomes and nanocapsules were prepared using the reverse-phase evaporation and nanoprecipitation methods, respectively. The particle size of the formulation ranged from 121.81 to 310.73 nm, the polydispersity index from 0.096 to 0.303, the zeta potential from -11.94 to -34.50 mV, the pH from 5.31 to 7.38, the drug content from 80.82 to 94.36 %, and the association efficiency was 98 %. Paroxetine hydrochloride showed slower release when associated with liposomes (43.82 %) compared to nanocapsules (95.59 %) after 10 h. In Vero cells, in vitro toxicity showed a concentration-dependent effect for paroxetine hydrochloride nanostructures. Both nanostructures decreased the immobility time in the TST at 2.5 mg/kg without affecting the number of crossings in the open field test, suggesting the antidepressant-like effect of paroxetine. In addition, the nanocapsules decreased the number of groomings, reinforcing the anxiolytic effect of this drug. These results suggest that the nanostructures were effective in preserving the antidepressant-like effect of paroxetine hydrochloride even at low doses.


Subject(s)
Liposomes , Nanocapsules , Paroxetine , Animals , Paroxetine/administration & dosage , Paroxetine/pharmacology , Paroxetine/chemistry , Nanocapsules/chemistry , Mice , Chlorocebus aethiops , Male , Vero Cells , Particle Size , Drug Liberation , Depression/drug therapy , Hindlimb Suspension , Antidepressive Agents/administration & dosage , Antidepressive Agents/chemistry , Antidepressive Agents/pharmacology , Antidepressive Agents, Second-Generation/administration & dosage , Antidepressive Agents, Second-Generation/chemistry , Antidepressive Agents, Second-Generation/pharmacology , Behavior, Animal/drug effects , Cell Survival/drug effects
9.
Pharmaceutics ; 16(6)2024 Jun 18.
Article in English | MEDLINE | ID: mdl-38931948

ABSTRACT

Nanocapsules provide selective delivery and increase the bioavailability of bioactive compounds. In this study, we examined the anticancer and immunomodulatory potential of Fridericia chica (crajiru) extract encapsulated in nanocapsules targeting myeloid leukemias. Nanocapsules containing crajiru (nanocapsules-CRJ) were prepared via interfacial polymer deposition and solvent displacement. Size and polydispersity were measured by dynamic light scattering. Biological assays were performed on leukemia cell lines HL60 and K562 and on non-cancerous Vero cells and human PBMC. The anticancer activity was evaluated using cytotoxicity and clonogenic assays, while the immunomodulatory activity was evaluated by measuring the levels of pro- and anti-inflammatory cytokines in PBMC supernatants treated with concentrations of nanocapsules-CRJ. Nanocapsules-CRJ exhibited significant cytotoxic activity against HL60 and K562 cells at concentrations ranging from 0.75 to 50 µg/mL, with the greatest reductions in cell viability observed at 50 µg/mL (p < 0.001 for HL60; p < 0.01 for K562), while not affecting non-cancerous Vero cells and human PBMCs. At concentrations of 25 µg/mL and 50 µg/mL, nanocapsules-CRJ reduced the formation of HL60 and K562 colonies by more than 90% (p < 0.0001). Additionally, at a concentration of 12 µg/mL, nanocapsules-CRJ induced the production of the cytokines IL-6 (p = 0.0002), IL-10 (p = 0.0005), IL-12 (p = 0.001), and TNF-α (p = 0.005), indicating their immunomodulatory potential. These findings suggest that nanocapsules-CRJ hold promise as a potential therapeutic agent with both cytotoxic and immunomodulatory properties.

10.
Nanomedicine (Lond) ; 2024 May 01.
Article in English | MEDLINE | ID: mdl-38690778

ABSTRACT

Aim: The present study investigated renal elimination after intravenous administration of four different formulations of lipid nanocapsules (LNCs) containing dyes adapted to Förster resonance energy transfer (FRET-LNCs). Materials & methods: FRET-LNCs of 85 or 50 nm with or without a pegylated surface were injected and collected in the blood or urine of rats at different time points. Quantitative analysis was performed to measure intact FRET-LNCs. Results & conclusion: No intact LNCs were found in urine (0 particles/ml) for all formulations. The 50-nm pegylated LNCs were eliminated faster from the blood, whereas 85-nm pegylated LNCS were eliminated slower than nonpegylated LNCs. Elimination of FRET-LNCs was mainly due to liver tissue interaction and not renal elimination.

11.
Article in English | MEDLINE | ID: mdl-38767313

ABSTRACT

Feed costs present a major burden in animal production for human consumption, representing a key opportunity for cost reduction and profit improvement. Nanotechnology offers potential to increase productivity by creating higher-quality and safer products. The feed sector has benefited from the use of nanosystems to improve the stability and bioavailability of feed ingredients. The development of nanotechnology products for feed must consider the challenges raised by biological barriers as well as regulatory requirements. While some nanotechnology-based products are already commercially available for animal production, the exponential growth and application of these products requires further research ensuring their safety and the establishment of comprehensive legislative frameworks and regulatory guidelines. Thus, this article provides an overview of the current state of the art regarding nanotechnology solutions applied in feed, as well as the risks and opportunities aimed to help researchers and livestock producers.

12.
Nanomicro Lett ; 16(1): 204, 2024 May 29.
Article in English | MEDLINE | ID: mdl-38811461
13.
ADMET DMPK ; 12(2): 299-317, 2024.
Article in English | MEDLINE | ID: mdl-38720922

ABSTRACT

Background and purpose: The employment of yeasts for biomedical purposes has become increasingly frequent for the delivery of prophylactic and therapeutic products. Its structural components, such as ß-glucans, mannan, and chitin, can be explored as immunostimulators that show safety and low toxicity. Besides, this system minimizes antigen degradation after administration, facilitating the delivery to the target cells. Review approach: This review sought to present molecules derived from yeast, called yeast shells (YS), and their applications as carrier vehicles for drugs, proteins, and nucleic acids for immunotherapy purposes. Furthermore, due to the diversity of information regarding the production and immunostimulation of these compounds, a survey of the protocols and immune response profiles generated was presented. Key results: The use of YS has allowed the development of strategies that combine efficiency and effectiveness in antigen delivery. The capsular structure can be recognized and phagocytized by dendritic cells and macrophages. In addition, the combination with different molecules, such as nanoparticles or even additional adjuvants, improves the cargo loading, enhancing the system. Activation by specific immune pathways can also be achieved by different administration routes. Conclusion: Yeast derivatives combined in different ways can increase immunostimulation, enhancing the delivery of medicines and vaccine antigens. These aspects, combined with the simplicity of the production steps, make these strategies more accessible to be applied in the prevention and treatment of various diseases.

14.
Int J Pharm ; 659: 124237, 2024 Jun 25.
Article in English | MEDLINE | ID: mdl-38762167

ABSTRACT

Intranasal administration is an efficient strategy for bypassing the BBB, favoring drug accumulation in the brain, and improving its efficiency. Lipid nanocapsules (LNC) are suitable nanocarriers for the delivery of lipophilic drugs via this route and can be used to encapsulate lipophilic molecules such as retinoic acid (RA) and calcitriol (Cal). As the hallmarks of multiple sclerosis (MS) are neuroinflammation and oligodendrocyte loss, our hypothesis was that by combining two molecules known for their pro-differentiating properties, encapsulated in LNC, and delivered by intranasal administration, we would stimulate oligodendrocyte progenitor cells (OPC) differentiation into oligodendrocytes and provide a new pro-remyelinating therapy. LNC loaded with RA (LNC-RA) and Cal (LNC-Cal) were stable for at least 8 weeks. The combination of RA and Cal was more efficient than the molecules alone, encapsulated or not, on OPC differentiation in vitro and decreased microglia cell activation in a dose-dependent manner. After the combined intranasal administration of LNC-RA and LNC-Cal in a mouse cuprizone model of demyelination, increased MBP staining was observed in the corpus callosum. In conclusion, intranasal delivery of lipophilic drugs encapsulated in LNC is a promising strategy for myelinating therapies.


Subject(s)
Administration, Intranasal , Calcitriol , Cell Differentiation , Nanocapsules , Oligodendrocyte Precursor Cells , Tretinoin , Animals , Tretinoin/administration & dosage , Tretinoin/pharmacology , Cell Differentiation/drug effects , Calcitriol/administration & dosage , Calcitriol/pharmacology , Oligodendrocyte Precursor Cells/drug effects , Mice , Mice, Inbred C57BL , Lipids/chemistry , Cells, Cultured , Male
15.
Talanta ; 276: 126273, 2024 Aug 15.
Article in English | MEDLINE | ID: mdl-38776775

ABSTRACT

Ultrasensitive and rapid detection of low concentration of Escherichia coli O157: H7 (E. coli O157:H7) in food is essential for food safety and public health. In this study, A novel fluorescence signal amplification biosensor based on magnetic separation platform and red fluorescent carbon dots (R-CDs)-encapsulated breakable organosilica nanocapsules (BONs) for ultrasensitive detection of E. coli O157:H7 was established. Wulff-type boronic acid functionalized magnetic nanoparticles (MNPs@B-N/APBA) with broad-spectrum bacterial recognition ability were synthesized for the first time to recognize and capture E. coli O157: H7 in food samples. R-CDs@BONs labeled with anti-E. coli O157:H7 monoclonal antibody (mAb@R-CDs@BONs-NH2) were used as the second recognition element to ensure the specificity for E. coli O157:H7 and form MNPs@B-N/APBA∼ E. coli O157:H7∼mAb@R-CDs@BONs-NH2 sandwich complexes, followed by releasing R-CDs to generate amplified fluorescence response signals for quantitative detection of E. coli O157:H7. The proposed method had a limit of detection with 25 CFU/mL in pure culture and contaminated lettuce samples, which the whole detection process took about 120 min. This fluorescence signal amplification biosensor has the potential to detect other pathogens in food by altering specific antibodies.


Subject(s)
Biosensing Techniques , Carbon , Escherichia coli O157 , Quantum Dots , Escherichia coli O157/isolation & purification , Biosensing Techniques/methods , Carbon/chemistry , Quantum Dots/chemistry , Nanocapsules/chemistry , Fluorescent Dyes/chemistry , Fluorescence , Limit of Detection , Organosilicon Compounds/chemistry , Food Microbiology , Lactuca/microbiology , Lactuca/chemistry
16.
Phytomedicine ; 130: 155763, 2024 Jul 25.
Article in English | MEDLINE | ID: mdl-38820661

ABSTRACT

BACKGROUND: Emodin is a chemical compound found in traditional Chinese herbs. It possesses anti-inflammatory and many other pharmacological effects. Our previous study showed that emodin significantly alleviates the inflammation effect of severe acute pancreatitis (SAP). However, its poor solubility, high toxicity and limited pancreas retention time hinder its clinical application. PURPOSE: We aimed to prepare emodin nanocapsules with improved bioavailability to achieve the controlled release of emodin by targeting macrophages. Further, the mechanism of mannose-conjugated chitosan-coated lipid nanocapsules loaded with emodin (M-CS-E-LNC) in the treatment of SAP was explored. METHODS: M-CS-E-LNC were prepared by the phase inversion method with slight modification. The expression of inflammation mediators and the anti-inflammation efficacy of M-CS-E-LNC were examined by ELISA, IHC and IF in macrophage cells and LPS-induced SAP mice. IVIS spectrum imaging and HPLC were applied to explore the controlled release of M-CS-E-LNC in the pancreas. LC-MS/MS was performed for lipidomics analysis of macrophages. Moreover, a vector-based short hairpin RNA (shRNA) method was used to silence CTP1 gene expression in macrophage cells. RESULTS: The levels of inflammatory mediators in macrophages were markedly decreased after treatment with M-CS-E-LNC. The same anti-inflammation effects were detected in SAP mouse through the analysis of serum levels of amylase, TNF-α and IL-6. Importantly, M-CS-E-LNC allowed the emodin to selectively accumulate at pancreas and gastrointestinal tissues, thus exhibiting a targeted release. Mechanistically, the M-CS-E-LNC treatment group showed up-regulated expression of the carnitine palmitoyltransferase 1 (CPT1) protein which promoted intracellular long-chain fatty acid transport, thereby promoting the M2 phenotype polarization of macrophages. CONCLUSION: M-CS-E-LNC exhibited significantly improved bioavailability and water solubility, which translated to greater therapeutic effects on macrophage polarization. Our findings also demonstrate, for the first time, that CPT1 may be a new therapeutic target for SAP treatment.


Subject(s)
Emodin , Lipid Metabolism , Macrophages , Nanocapsules , Pancreatitis , Animals , Emodin/pharmacology , Mice , Macrophages/drug effects , Macrophages/metabolism , Pancreatitis/drug therapy , RAW 264.7 Cells , Lipid Metabolism/drug effects , Male , Anti-Inflammatory Agents/pharmacology , Chitosan/pharmacology , Chitosan/chemistry , Mice, Inbred C57BL , Lipopolysaccharides , Metabolic Reprogramming
17.
Pharmaceuticals (Basel) ; 17(4)2024 Apr 10.
Article in English | MEDLINE | ID: mdl-38675445

ABSTRACT

Lidocaine is the most commonly used local anesthetic worldwide, known for its rapid onset and moderate duration of anesthesia. However, it is short-lived and does not effectively promote effective topical anesthesia in the oral cavity when used alone. Our aim was to investigate whether an approximate 50% encapsulation of lidocaine in poly(ε-caprolactone) nanocapsules (LDC-Nano) would be able to increase its permeation and analgesic efficacy and reduce cytotoxicity. In this study, we characterized LDC-Nano and conducted MTT tests with HaCaT cells to assess their in vitro cytotoxicity. Additionally, in vitro permeation assays across the pig esophageal epithelium and the anesthetic efficacy of the hind paw incision model in rats were performed. Plain lidocaine (LDC) was compared with LDC-Nano and lidocaine hydrochloride plus epinephrine (LDC-Epi). The physicochemical characteristics of LDC-Nano were satisfactory (pH: 8.1 ± 0.21; polydispersity index: 0.08 ± 0.01; mean diameter (nm): 557.8 ± 22.7; and encapsulation efficiency (%): 51.8 ± 1.87) and remained stable for up to 4 months. LDC-Nano presented similar in vitro cytotoxicity to LDC but was higher than LDC-Epi (LD50: LDC = 0.48%; LDC-Nano = 0.47%; and LDC-Epi = 0.58%; p < 0.0001). Encapsulation increased the permeability coefficient about 6.6 times and about 7.5 the steady-state flux of lidocaine across the mucosal epithelium. Both encapsulation and epinephrine improved anesthesia duration, with epinephrine demonstrating superior efficacy (100% of animals were anesthetized up to 100, 30, and 20 min when LDC-Epi, LDC-nano, and LDC were used, respectively). Although LDC-Epi demonstrated superior in vivo anesthetic efficacy, the in vitro permeation and cytotoxicity of LDC-Nano indicate promising avenues for future research, particularly in exploring its potential application as a topical anesthetic in the oral cavity.

18.
Biomed Pharmacother ; 174: 116308, 2024 May.
Article in English | MEDLINE | ID: mdl-38626517

ABSTRACT

The kernel oil of the Attalea phalerata Mart. Ex Spreng (Acurí) is traditionally used in several Latin American countries to treat respiratory problems, inflammation, and fever. However, it cannot be found on the literature any attend to use this oil in pharmaceutical formulation. In this paper, it was developed Acurí oil-loaded nanocapsules, and it was evaluated the cytotoxicity against cancer cells, the antinflammatory activity and the oral acute toxicity in rats. Acurí oil contains lauric acid as the predominant saturated fatty acid (433.26 mg/g) and oleic acid as the main unsaturated fatty acid (180.06 mg/g). The Acurí oil-loaded nanocapsules showed a size of 237 nm, a polydispersity index of 0.260, and a high ζ-potential of -78.75 mV. It was obtained an encapsulation efficiency of 88.77%, and the nanocapsules remain stable on the shelf for 180 days. The nanocapsules showed a rapid release profile (98.25% in 40 minutes). Nanocapsules at a dose of 10 mg/kg exhibit an anti-inflammatory effect similar to indomethacin at the same dose. The nanocapsules showed excellent antiproliferative effect and selectivity index against prostate tumor cells (IC50 2.09 µg/mL, SI=119.61) and kidney tumor cells (IC50 3.03 µg/mL, SI=82.50). Both Acurí oil and Acurí oil-loaded nanocapsules are nontoxic at a dose of 2000 mg/kg. Additionally, they reduce serum triglyceride and total cholesterol levels in rat and could find application in nutraceutical formulations. The Acurí oil-loaded nanocapsules emerge as a promising candidate for new antitumor therapies.


Subject(s)
Anti-Inflammatory Agents , Nanocapsules , Plant Oils , Animals , Anti-Inflammatory Agents/pharmacology , Anti-Inflammatory Agents/isolation & purification , Anti-Inflammatory Agents/administration & dosage , Plant Oils/pharmacology , Male , Humans , Rats , Rats, Wistar , Administration, Oral , Cell Line, Tumor
19.
ACS Nano ; 18(17): 11300-11310, 2024 Apr 30.
Article in English | MEDLINE | ID: mdl-38637969

ABSTRACT

The fast-charging performance of conventional lithium-ion batteries (LIBs) is determined by the working temperature. LIBs may fail to work under harsh conditions, especially in the low-temperature range of the local environment or in the high-temperature circumstances resulting from the release of substantial Joule heating in the short term. Constructing a thermal engineering framework for thermal regulation and maintaining the battery running at an appropriate temperature range are feasible strategies for developing temperature-tolerant, fast-charging LIBs. In this work, we prepare phase change nanocapsules as a thermal regulating layer on the cell surface. The polyurea shells of the nanocapsules are decorated with polyaniline, where the molecular vibration of polyaniline is enhanced under solar irradiation, enabling light-to-heat conversion that achieves an effective temperature increment at low temperatures. Based on the large latent heat storage capability of the n-octadecane core in the nanocapsules, the thermal regulating layer is sufficient to modulate strong heat release when operating LIBs at a high current rate, which efficiently prevents strong side reactions at high temperatures or even the occurrence of thermal runaway. This work highlights the promise of optimizing the operating temperature with a thermal regulator to ensure the safety and performance stability of fast-charging LIBs.

20.
J Control Release ; 369: 658-667, 2024 May.
Article in English | MEDLINE | ID: mdl-38604384

ABSTRACT

Granzyme B (GrB)-based immunotherapy is of interest for cancer treatment. However, insufficient cellular uptake and a lack of targeting remain challenges to make use of GrB for solid tumour therapy. As GrB induced cell death requires the help of perforin (PFN), we designed a system (nGPM) for the co-delivery of GrB and PFN. Therefore, GrB and PFN were loaded in a porous polymeric nanocapsule rich in acetylcholine analogues and matrix metalloproteinase-2 (MMP-2) responsive peptides. The neutrally charged nGPM nanocapsules showed as long circulating time and accumulated at the tumour sites. Once in the tumour the outside shell of nanocapsules became degraded by overexpressed MMP-2 proteases, resulting in the release of GrB and PFN. We found that the PFN complex formed small pores on the surface of tumour cells which allow GrB to enter the cytoplasm of tumour cells inducing cell apoptosis and tumour suppression significantly.


Subject(s)
Granzymes , Nanocapsules , Perforin , Granzymes/metabolism , Nanocapsules/chemistry , Animals , Perforin/metabolism , Humans , Cell Line, Tumor , Neoplasms/drug therapy , Neoplasms/therapy , Neoplasms/immunology , Apoptosis/drug effects , Matrix Metalloproteinase 2/metabolism , Immunotherapy/methods , Mice, Inbred BALB C , Female , Mice
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