Dry powder inhalation for sildenafil citrate: formulation and performance tests Taízia Dutra Silva, Ana Carolina Guimarães Ribeiro, Raquel Braga Dutra Gonçalves, Jackson Antonio Lamounier Camargos Resende, Cristina Duarte Vianna-Soares Brazilian Journal of Pharmaceutical Sciences, 2026 Pulmonary arterial hypertension (PAH) is a severe disease responsible for high mortality in the affected population. Due to the limitations in treatment as severe adverse effects, high cost, we aimed to develop a simple therapeutic option for pulmonary administration, using a vasodilator sildenafil citrate (SILC) in a dry powder inhalation using lactose as carrier. A formulation of micronized SILC was prepared after 30 min wet grinding of the active with the aid of a vibration shear-mill. Solid characterization by laser diffraction and X-ray powder diffraction was assessed for active. Performance tests such as delivered-dose uniformity (DDU) and aerodynamic particle size distribution (APSD), using Dosage Unit Sampling Apparatus and Andersen Cascate Impactor, respectively, were performed. The micronization of SILC resulted in a medium size of 4.54 μm and a 50th percentile of 2.93 μm. For DDU, the total amount delivered ranged from 92.42 to 109.05% of the targeted dose, in agreement with the specified range (75.0-125.0%). For ASPD, a fine particle fraction of 35% was satisfactorily obtained. This formulation is simple and promising therapeutic option for the treatment of PAH with the advantage of being easily produced using less complex carrier matrix or equipment, in a short time.
Phagocytosis Modulated by a PtII Complex with Triphenylphosphine and 5-Heptyl-1,3,4-oxadiazole-2-(3H)-thione in a Microemulsion System Bruna A. Rodrigues, Angelina M. de Almeida, Mauro V. de Almeida, Jackson Antônio L. C. Resende, Wendell Guerra, et al. Journal of the Brazilian Chemical Society, 2026 In this work, the trans-[Pt(L)2(PPh3)2] complex (L: 5-heptyl-1,3,4-oxadiazole-2-(3H)-thione) was associated with a microemulsion (ME/PtII complex). The microemulsified system underwent physicochemical characterization, including pH, conductivity, rheology, zeta potential, and dynamic light scattering (DLS) measurements. The microemulsion system remained stable at a pH near 6.0, indicating biocompatibility, while the conductivity was between 7 and 8 μS cm-1 , with a hysteresis area of −0.06 Pas-1 for the ME/PtII complex. The DLS technique confirmed the presence of a microemulsion with particle sizes ranging from 10 to 200 nm. The polydispersity index for the ME/PtII complex system was close to 0.3, indicating a monodisperse system, with a zeta potential of −19.2 ± 4.49 mV. These results showed that the system containing the PtII complex and the microemulsion is thermodynamically stable. Subsequently, cell viability studies demonstrated that the ME/PtII complex system is not toxic to peripheral blood mononuclear cells (PBMCs). In the phagocytosis activity assay, the complex associated with the microemulsion showed an increase in the phagocytosis index, suggesting that the microemulsion (ME/PtII complex) has potential for new biological assays, such as antitumor and antibacterial.
Green Synthesis of Spiro Compounds with Potential Anticancer Activity through Knoevenagel/Michael/Cyclization Multicomponent Domino Reactions Organocatalyzed by Ionic Liquid and Microwave-Assisted Regina Westphal, Eclair Venturini Filho, Laiza Bruzadelle Loureiro, Cláudio Francisco Tormena, Claudia Pessoa, et al. Molecules, 2022 In this work a microwave-assisted Knoevenagel/Michael/cyclization multicomponent domino methodology, using ethanol as solvent and the ionic liquid 1-methylimidazolium chloride as catalyst was developed for the synthesis of spiro compounds. The reaction conditions considered ideal were determined from a methodological study varying solvent, catalyst, amount of catalyst, temperature, and heating mode. Finally, the generality of the methodology was evaluated by exploring the scope of the reaction, varying the starting materials (isatin, malononitrile, and barbituric acid). Overall, the twelve spiro compounds were synthesized in good yields (43–98%) and the X-ray structure of compound 1b was obtained. In addition, the in vitro antiproliferative activities of the spirocycles against four types of human cancer cell lines including HCT116 (human colon carcinoma), PC3 (prostate carcinoma), HL60 (promyelocytic leukemia), and SNB19 (astrocytoma) were screened by MTT-based assay. It is noteworthy that spiro compound 1c inhibited the four cell lines tested with the lowest IC50 values: 52.81 µM for HCT116, 74.40 µM for PC3, 101 µM for SNB19, and 49.72 µM for HL60.
Absolute configuration of clemateol Marcelo Pedroso, Adriana Gehn, Mateus Stivanin, Enrique Larghi, Robert Burrow, et al. Journal of the Brazilian Chemical Society, 2018
21α-fluoro-7-nor-12,13,15,16-tetrahydrovouacapane-17β, 21α-lactone Silvana Guilardi, Jackson Antônio Lamounier Camargos Resende, Maria Teresa do Prado Gambardella, Antonio Jacinto Demuner, Luis Claudio de Almeida Barbosa, et al. Acta Crystallographica Section E Structure Reports Online, 2003
2-Cyano-N-(2-hydroxyphenyl)acetamide Jackson Antônio Lamounier Camargos Resende, Sauli Santos Jr, Javier Ellena, Silvana Guilardi Acta Crystallographica Section E Structure Reports Online, 2003
Redetermination of nickel bis(dithiocarbamate) at 100 K Sauli Santos, Silvana Guilardi, Jackson A. L. C. Resende, Mayura M. M. Rubinger, Marcelo R. L. Oliveira, et al. Acta Crystallographica Section E Structure Reports Online, 2003
RECENT SCHOLAR PUBLICATIONS
Phagocytosis Modulated by a Pt II Complex with Triphenylphosphine and 5-Heptyl-1,3,4-oxadiazole-2-(3 H )-thione in a Microemulsion System BA Rodrigues, AM Almeida, MV Almeida, JALC Resende, W Guerra, ... Journal of the Brazilian Chemical Society 37, e-20250185 , 2026 2026
Novel Copper (II) Complexes Containing β-Diketones and Imines as Ligands Modulate the Expression of lncRNAs in Triple-Negative Breast Cancer Cells GG Rocha, LMS Ramos, LAS Barbosa, RP Siqueira, FC da Silva, ... ACS omega 11 (1), 687-699 , 2025 2025
Experimental Electron Density Analysis of the Reaction Steps Leading to Coordination of 1-Phenyl-1H-1, 2, 3-Triazole-4-Carboxylic Acid to Copper (II) MCR Freitas, WBS Braga, LHR Dos Santos, NA Rey, JALC Resende, ... The Journal of Physical Chemistry A 129 (51), 11848-11860 , 2025 2025
Structural and photophysical properties of a two-dimensional europium (III) coordination network with a diyne-based ligand CRMO Matos, MOB de Sousa, CBP Ligiero, HCS Junior, GB Ferreira, ... Journal of Molecular Structure, 144560 , 2025 2025 Citations: 1
Possibilidades de aplicação de água de reuso proveniente de condicionadores de ar baseadas em análises físico-químicas UM de Alencar, RMP Dantas, WB dos Santos, JALC Resende, ... RCT-Revista de Ciência e Tecnologia 11 , 2025 2025
Arylboronic acids as safe and specific human butyrylcholinesterase inhibitors EM dos Santos, NAA e Silva, KG Gonçalves, AAM Vale, ... Journal of Molecular Structure 1290, 135932 , 2023 2023 Citations: 5
Synthesis, characterization and computational investigation of the phosphatase activity of a dinuclear Zinc (II) complex containing a new heptadentate asymmetric ligand LMO Costa, IS Reis, C Fernandes, MM Marques, JALC Resende, ... Journal of Inorganic Biochemistry 239, 112064 , 2023 2023 Citations: 2
Characterization of Portland cement pastes with silica addition aiming at Cr (VI) immobilization CAM Moura, JALC Resende, KC Souza Ambiente Construído 23, 245-261 , 2023 2023 Citations: 1
Synthesis and in vitro evaluation of antimycobacterial activity of two palladium (II) complexes based on 5-alkyl-1, 3, 4-oxadiazol-2 (3H)-thione derivatives WA Souza, FM Demarqui, AM de Almeida, RTC Silva, DA Alves, ... Journal of Molecular Structure 1270, 133888 , 2022 2022 Citations: 6
Preparation, cytotoxic activity and DNA interaction studies of new platinum (II) complexes with 1, 10-phenanthroline and 5-alkyl-1, 3, 4-oxadiazol-2 (3H)-thione derivatives WA Souza, LMS Ramos, AM de Almeida, DY Tezuka, CD Lopes, ... Journal of Inorganic Biochemistry 237, 111993 , 2022 2022 Citations: 15
Green synthesis of spiro compounds with potential anticancer activity through Knoevenagel/Michael/cyclization multicomponent domino reactions organocatalyzed by ionic liquid … R Westphal, E Venturini Filho, LB Loureiro, CF Tormena, C Pessoa, ... Molecules 27 (22), 8051 , 2022 2022 Citations: 21
A New Saquinavir Mesylate-Sodium Decyl Sulfate Salt Discovered by Serendipity during an Anomalous Dissolution Test: Fandaruff et al. C Fandaruff, T Caon, AM Araya-Sibaja, GS Rauber, MAS Silva, ... Pharmaceutical Research 39 (1), 189-200 , 2022 2022
Synthesis and in vitro and in silico studies of 1H-and 2H-1, 2, 3-triazoles as antichagasic agents TB Silva, KNK Ji, FP Pauli, RMS Galvão, AFM Faria, ML Bello, ... Bioorganic Chemistry 116, 105250 , 2021 2021 Citations: 24
Chemistry and anti-herpes simplex virus type 1 evaluation of 4-substituted-1 H -1,2,3-triazole-nitroxyl-linked hybrids AC Cunha, VF Ferreira, MGF Vaz, RAA Cassaro, JALC Resende, ... Molecular Diversity 25 (4), 2035-2043 , 2021 2021 Citations: 18
(Phenylamino) pyrimidine-1, 2, 3-triazole derivatives as analogs of imatinib: searching for novel compounds against chronic myeloid leukemia LCF Pimentel, LVB Hoelz, HF Canzian, FSC Branco, AP de Oliveira, ... Beilstein Journal of Organic Chemistry 17 (1), 2260-2269 , 2021 2021 Citations: 10
Semisynthesis of dolabellane diterpenes: Oxygenated analogues with increased activity against Zika and Chikungunya viruses F Amaya García, C Cirne-Santos, C de Souza Barros, AM Pinto, ... Journal of natural products 84 (4), 1373-1384 , 2021 2021 Citations: 11
Effect of the hydroxamate group in the antitumoral activity and toxicity toward normal cells of new copper (II) complexes NFB Azeredo, FV Borges, MS Mathias, JALC Resende, RWA Franco, ... BioMetals 34 (2), 229-244 , 2021 2021 Citations: 11
Crystal structure and spectroscopy properties of new PtII complexes containing 5-alkyl-1, 3, 4-oxadiazol-2-thione derivatives WA Souza, AM de Almeida, M Pivatto, MV de Almeida, GP Guedes, ... Journal of Molecular Structure 1226, 129250 , 2021 2021 Citations: 12
NOVAS PERSPECTIVAS QUIMIOTERÁPICAS ANTI-TRYPANOSOMA CRUZI IN VITRO DE COMPOSTOS DE COORDENAÇÃO DINUCLEARES DE Fe (III) COM ATIVIDADE NANOMOLAR FF Moreira, J de Araujo Portes, C Fernandes, AH Júnior, JALC Resende, ... Congresso Fluminense de Pós-Graduação-CONPG , 2021 2021
Development of new dinuclear Fe (III) coordination compounds with in vitro nanomolar antitrypanosomal activity FF Moreira, J de Araujo Portes, NFB Azeredo, C Fernandes, A Horn, ... Dalton Transactions 50 (35), 12242-12264 , 2021 2021 Citations: 14
MOST CITED SCHOLAR PUBLICATIONS
Synthesis of new 9-hydroxy-alpha- and 7-hydroxy-beta-pyran naphthoquinones and cytotoxicity against cancer cell lines DR da Rocha, ACG de Souza, JALC Resende, WC Santos, ... ORGANIC & BIOMOLECULAR CHEMISTRY 9 (11), 4315-4322 , 2011 2011 Citations: 72
An insight into carvedilol solid forms: effect of supramolecular interactions on the dissolution profiles LD Prado, HVA Rocha, JALC Resende, GB Ferreira, ... CrystEngComm 16 (15), 3168-3179 , 2014 2014 Citations: 61
Dolabelladienols A–C, New Diterpenes Isolated from Brazilian Brown Alga Dictyota pfaffii A Pardo-Vargas, IB Oliveira, PRS Stephens, CC Cirne-Santos, ... Marine Drugs 12 (7), 4247-4259 , 2014 2014 Citations: 60
In vitro and in vivo studies of the antineoplastic activity of copper (II) compounds against human leukemia THP-1 and murine melanoma B16-F10 cell lines LJH Borges, ÉS Bull, C Fernandes, A Horn Jr, NF Azeredo, ... European journal of medicinal chemistry 123, 128-140 , 2016 2016 Citations: 51
Preparation and characterization of solid dispersion of simvastatin TD Silva, VT Arantes, VT (Arantes, JALC Resende, JALC (Resende, ... DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY 36 (11), 1348-13 , 2010 2010 Citations: 51
Pseudopolymorphs and intrinsic dissolution of nevirapine BG Pereira, FD Fonte-Boa, JALC Resende, CB Pinheiro, NG Fernandes, ... CRYSTAL GROWTH & DESIGN 7 (10), 2016-2023 , 2007 2007 Citations: 51
Synthesis and evaluation of copper (II) complexes with isoniazid-derived hydrazones as anticancer and antitubercular agents GSS Firmino, MVN de Souza, C Pessoa, MCS Lourenco, JALC Resende, ... BioMetals 29 (6), 953-963 , 2016 2016 Citations: 49
Cobalt lawsone complexes: searching for new valence tautomers MA RIBEIRO, M Lanznaster, M Lanznaster, MMP Silva, JALC RESENDE, ... DALTON TRANSACTIONS 42 (15), 5462-5470 , 2013 2013 Citations: 46
New oxirane derivatives of 1,4-naphthoquinones and their evaluation against T. cruzi epimastigote forms PF Carneiro, SB do Nascimento, AV Pinto, MCFR Pinto, GC Lechuga, ... BIOORGANIC & MEDICINAL CHEMISTRY 20 (16), 4995-5000 , 2012 2012 Citations: 46
Synthesis and antimalarial activity of quinones and structurally-related oxirane derivatives PF Carneiro, MCRF Pinto, RKF Marra, FC da Silva, JALC Resende, ... European Journal of Medicinal Chemistry 108, 134-140 , 2016 2016 Citations: 44
Synthesis and antimicrobial evaluation of promising 7-arylamino-5, 8-dioxo-5, 8-dihydroisoquinoline-4-carboxylates and their halogenated amino compounds for treating Gram … JS Novais, VR Campos, ACJA Silva, MCBV de Souza, VF Ferreira, ... RSC advances 7 (30), 18311-18320 , 2017 2017 Citations: 40
Synthesis and Characterization of LiCoO 2 from Different Precursors by Sol-Gel Method BGA Freitas, JM Siqueira Jr, LM Costa, GB Ferreira, JALC Resende Journal of the Brazilian Chemical Society 28 (11), 2254-2266 , 2017 2017 Citations: 38
Induction of apoptosis in leukemia cell lines by new copper (II) complexes containing naphthyl groups via interaction with death receptors C Fernandes, A Horn Jr, BF Lopes, ES Bull, NFB Azeredo, MM Kanashiro, ... Journal of inorganic biochemistry 153, 68-87 , 2015 2015 Citations: 37
Determination of the relevant magnetic interactions in low-dimensional molecular materials: the fundamental role of single crystal high frequency EPR RA Allao, AK Jordao, JALC Resende, AC Cunha, VF Ferreira, MA Novak, ... DALTON TRANSACTIONS 40 (41), 10843-10850 , 2011 2011 Citations: 37
A new mixed-valence Mn (II) Mn (III) compound with catalase and superoxide dismutase activities RO Costa, SS Ferreira, CA Pereira, JR Harmer, CJ Noble, G Schenk, ... Frontiers in chemistry 6, 491 , 2018 2018 Citations: 36
DNA binding, cleavage, apoptosis and cytotoxicity studies of three heteroleptic nickel complexes bearing β-diketones LM Sousa, WA Souza, DA Paixao, RB Fazzi, DY Tezuka, CD Lopes, ... Inorganica Chimica Acta 511, 119824 , 2020 2020 Citations: 34
Sesquiterpenes from the Brazilian red alga Laurencia dendroidea J. Agardh FL da Silva Machado, TLB Ventura, LM de Souza Gestinari, V Cassano, ... Molecules 19 (3), 3181 , 2014 2014 Citations: 33
Near infrared organic light emitting devices based on a new erbium (III) β-diketonate complex: Synthesis and optoelectronic investigations Z Ahmed, RE Aderne, J Kai, JALC Resende, HI Padilla-Chavarría, ... RSC advances 7 (30), 18239-18251 , 2017 2017 Citations: 32
A study on the properties and reactivity of naphthoquinone–cobalt (III) prototypes for bioreductive prodrugs FLS Bustamante, FS MIRANDA, FAV CASTRO, JALC RESENDE, ... Journal of Inorganic Biochemistry 132, 37-44 , 2014 2014 Citations: 32
Synthesis of New 2-Aminocarbohydrate-1,4-Naphthoquinone Derivatives Promoted by Ultrasonic Irradiation CFJ Franco, AK Jordão, VF Ferreira, AC Pinto, MCBV Souza, ... JOURNAL OF THE BRAZILIAN CHEMICAL SOCIETY 22 (1), 187-193 , 2011 2011 Citations: 30