Pharmaceutical Science, Drug Discovery, Pharmacology, Toxicology and Pharmaceutics
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Scopus Publications
Scopus Publications
Impact of nanostructured formulations for schistosomiasis treatment: a systematic review of in vivo preclinical evidence Laís de Castro Carvalho Silva, Luís Felipe Cunha dos Reis, Luiz Cosme Cotta Malaquias, Flávia Chiva Carvalho, Rômulo Dias Novaes, et al. Journal of Pharmacy and Pharmacology, 2025 Background Schistosomiasis is a neglected tropical disease caused by Schistosoma sp., and praziquantel (PZQ) is the first-line treatment. However, traditional PZQ formulations have low solubility and fast metabolism, limiting its effectiveness. Thus, nanoparticles have been proposed to improve the bioavailability and efficacy of poorly soluble antischistosomal drugs. Aims This systematic review used in vivo preclinical studies to map the available evidence and compare the efficacy of free PZQ and PZQ-based nanostructured formulations (N-PZQ) for schistosomiasis treatment. Methods PubMed, Embase, Scopus, and Web of Science were searched, and 1186 experimental studies published between 1974 and 2024 were screened. Parasitological, histopathological, pharmacokinetic, and toxicological outcomes were evaluated. Results Twelve relevant studies were identified exploring N-PZQ formulations based on liposomes, nanoliposomes, and nanocrystals. N-PZQ demonstrated better therapeutic efficacy than free PZQ, reducing parasite load, modifying oogram profiles, and down-regulating liver granuloma development (number and size). N-PZQ also exhibited improved pharmacokinetic profile, with enhanced bioavailability and longer half-life, as well as reduced toxicity (cytotoxicity, genotoxicity, and hepatotoxicity) compared to free PZQ. Conclusion PZQ-based nanostructured formulations represent a promising strategy to enhance schistosomiasis treatment by improving chemotherapy efficacy, optimizing antiparasitic responses, pharmacokinetics, and reducing drug toxicity.
Uptake and Inhibition of P-Glycoprotein-Mediated Efflux Evaluation of Encapsulated Methotrexate Chitosan and Hypromellose Phthalate Nanoparticles for Potential Glioblastoma Treatment Valéria de Moura Leite Naves, Rafaela Franco Dias Bruzadelli, Marisa Ionta, Maria Palmira Daflon Gremião, Liliane Neves Pedreiro, et al. Pharmaceutics, 2025 Background: Methotrexate (MTX), a folic acid antagonist used in chemotherapy, faces limitations due to cancer cell resistance, high toxicity, and low bioavailability. Objective: This study developed nanoparticles (NPs) of chitosan (QS) and hydroxypropylmethylcellulose phthalate (HPMCP) to encapsulate MTX for potential effect investigation on glioblastoma cell targeting and P-gp efflux inhibition. Method: NPs were produced by the polyelectrolyte complexation method and were characterized by DLS, PDI, DSC, FTIR, PXRD, MEV, drug release profile, and an in vitro mucoadhesion test. Cell viability, flow cytometry, and LSCM using U251MG (glioblastoma) and CCD 1059Sk (fibroblasts) cells were used to evaluate glioblastoma and the P-gp efflux effect. Results: NPPM29 (QS3:1) showed 91.72% encapsulation efficiency, a mean diameter of 452.6 nm, and a zeta potential of +22.5 mV. DSC, FTIR, and PXRD confirmed the QS-HPMCP supramolecular interaction. Liquid falling mucoadhesion tests demonstrated strong retention of NPPM29 (84%) compared to free MTX (10.5%). In vitro release studies indicated controlled drug release at pH 7.4. Cytotoxicity assays in U251MG revealed enhanced efficacy of NPPM29 (IC50 = 68.79 µg/mL) compared to free MTX (IC50 = 80.54 µg/mL), with minimal impact on fibroblasts, confirming tumor specificity. Flow cytometry and LSCM confirmed improved cellular internalization and P-gp inhibition. Conclusions: These findings highlight the potential of MTX-QS-HPMCP-NPs for glioblastoma therapy.
NLC-Based Sunscreen Formulations with Optimized Proportion of Encapsulated and Free Filters Exhibit Enhanced UVA and UVB Photoprotection Margarete M. de Araújo, Andressa C. Schneid, Mariana S. Oliveira, Samuel V. Mussi, Miller N. de Freitas, et al. Pharmaceutics, 2024 The topical use of sunscreens is recommended for avoiding the damaging effects of UV radiation. However, improvements are still needed in the existing products to enhance their photoprotection effectiveness and safety. This involves minimizing the use of chemical UV filters while providing enhanced and prolonged photoprotection. This work investigated novel sunscreen formulations and their UV protection effects by encapsulating Uvinul® A, Tinosorb® S, and Uvinul® T150 into nanostructured lipid carriers (NLCs) based on bacuri butter and raspberry seed oil. First, the impact of critical formulation and process parameters on NLCs’ particle size was evaluated using a 22 Face Centered Central Composite Design. Then, formulations were evaluated in terms of critical quality factors, in vitro skin permeation, and in vitro and in vivo photoprotection activities. The developed NLCs-containing formulations exhibited appropriate size (122–135 nm), PdI (<0.3), encapsulation efficiency (>90%), and drug content (>80%), which were preserved for at least 90 days under different stability conditions. Moreover, these NLCs-based formulations had equivalent skin permeation to emulsion-based controls, and the addition of NLCs into sunscreen cream bases in the optimum proportion of 20% (w/w) resulted in enhanced UVA and UVB photoprotection levels, despite a 10% reduction in the total filters content. Altogether, these results describe the application of nanoencapsulated organic UV filters in innovative sunscreen formulations to achieve superior photoprotection and cosmeceutical properties.
Evaluation of methotrexate-loaded surfactants, ceramides and cholesterol-based lamellar phases as a topical treatment for psoriasis Cintia Oliveira Alves, Rômulo Dias Novaes, Maria Tereza Carneiro Paschoal Bernardes, Reggiani Vilela Gonçalves, Laíla Pereira da Silva, et al. Journal of Pharmacy and Pharmacology, 2022 Objective Psoriasis is a chronic inflammatory skin disorder. Oral or subcutaneous methotrexate (MTX) is a first-line antipsoriatic treatment, whose adverse effects can be observed even at low doses. To minimize systemic side effects, antipsoriatic drugs should be administered topically, since they could permeate the stratum corneum. As liquid crystals with lamellar phase (LP) can be helpful in promoting skin permeation, this work evaluated two MTX-loaded LPs (C1CH and C1CHCE), based on stearic acid, cholesterol and ceramides, like topical treatments for mice with imiquimod-induced psoriasis. Methods C1CH and C1CHCE were topically administered to mice with imiquimod-induced psoriasis. Dexamethasone cream was used as positive treatment control. Skin histology and inflammation biomarkers were assessed. Key findings C1CH and C1CHCE exhibited marked immunomodulatory effects and induced extensive microstructural skin remodelling on the epidermis and dermis. These formulations increased keratinization score, epidermis thickness, inflammatory infiltrate, hair follicle hypertrophy and vascular congestion in the dermis. C1CH and C1CHCE also attenuated IL-10 upregulation and upregulated IL-1, IFN-γ, TNF-α and prostaglandin E2 levels, as well as myeloperoxidase, N-acetyl-β-d-glucosaminidase and cyclooxygenase 2 activity compared with untreated psoriatic animals. Conclusion Although liquid crystals have been reported as good options for carrying topical drugs, they need to be carefully assessed on a case-by-case basis.
Preclinical evaluation of polymeric nanocomposite containing pregabalin for sustained release as potential therapy for neuropathic pain Rafaela Figueiredo Rodrigues, Juliana Barbosa Nunes, Sandra Barbosa Neder Agostini, Paloma Freitas dos Santos, Juliana Cancino-Bernardi, et al. Polymers, 2021 This study offers a novel oral pregabalin (PG)-loaded drug delivery system based on chitosan and hypromellose phthalate-based polymeric nanocomposite in order to treat neuropathic pain (PG-PN). PG-PN has a particle size of 432 ± 20 nm, a polydispersity index of 0.238 ± 0.001, a zeta potential of +19.0 ± 0.9 mV, a pH of 5.7 ± 0.06, and a spherical shape. Thermal and infrared spectroscopy confirmed nanocomposite generation. PG-PN pharmacokinetics was studied after a single oral dose in male Wistar rats. PG-PN showed greater distribution and clearance than free PG. The antinociceptive effect of PG-PN in neuropathic pain rats was tested by using the chronic constriction injury model. The parameter investigated was the mechanical nociceptive threshold measured by the von Frey filaments test; PG-PN showed a longer antinociceptive effect than free PG. The rota-rod and barbiturate sleep induction procedures were used to determine adverse effects; the criteria included motor deficit and sedative effects. PG-PN and free PG had plenty of motors. PG-PN exhibited a less sedative effect than free PG. By prolonging the antinociceptive effect and decreasing the unfavorable effects, polymeric nanocomposites with pregabalin have shown promise in treating neuropathic pain.
Determination of dexamethasone acetate in CETETH 20-based in liquid crystalline systems using HPLC Márcia Helena Oyafuso, Bruno Fonseca‐Santos, Ana Carolina Kogawa, Flávia Chiva Carvalho, Maria Palmira Daflon Gremião, et al. Biomedical Chromatography, 2021 Dexamethasone acetate (DEX), a potent anti‐inflammatory, is used primarily in the treatment of inflammatory and autoimmune diseases. It was incorporated in CETETH 20 (polyoxyethylene 20 cetyl alcohol)–based liquid crystalline systems to enhance the purpose of the drug. Concomitant with the pharmaceutical technology performed, a HPLC method was developed and validated for the quantification of dexamethasone acetate in CETETH 20‐based liquid crystalline systems for the evaluation of the drug in the new matrix. The method was performed using a C18 column with acetonitrile:methanol:water (35:35:30, v/v/v) as the mobile phase at a flow rate of 0.8 mL min−1 at 239 nm. The method was linear in the range of 1–25 μg mL−1; the limit of quantification and limit of detection were 0.05 and 0.16 μg mL−1, respectively; the accuracy of the method was 99.92% (relative standard deviation < 1%), and it presented intra‐day and inter‐day precision with deviations less than 1%. In this context, the method was successfully used to determine the incorporation efficiency of DEX in CETETH 20‐based liquid crystalline systems and can be easily used by pharmaceutical companies and laboratories around the world.
Determination of the osmolarity of suspensions of methotrexate-loaded chitosan nanoparticles Revista De Ciencias Farmaceuticas Basica E Aplicada, 2017
Characterization of the bioadhesion and syringeability of systems based on surfactants and hydrogels Revista De Ciencias Farmaceuticas Basica E Aplicada, 2017
Obtaining poloxamer-based thermoresponsive systems and characterization of gelation and syringeability Revista De Ciencias Farmaceuticas Basica E Aplicada, 2017
Phase behavior of surfactant-based systems as potential vehicles for methotrexate uptake in the topical treatment of psoriasis Revista De Ciencias Farmaceuticas Basica E Aplicada, 2017
Mucoadhesive drug delivery systems Flávia Chiva Carvalho, Marcos Luciano Bruschi, Raul Cesar Evangelista, Maria Palmira Daflon Gremião Brazilian Journal of Pharmaceutical Sciences, 2010
