Prospecting for Active Compounds in Medicinal Chemistry and Pharmaceutical Technological Development

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Pharmaceutical Technology, Manufacturing and Devices".

Deadline for manuscript submissions: closed (31 December 2022) | Viewed by 9207

Special Issue Editors


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Laboratório de Desenvolvimento e Ensaios de Medicamentos, Centro de Ciências Biológicas e da Saúde, Universidade Estadual da Paraíba, 351, Cidade Universitária, Campina Grande 58429-500, PB, Brazil
Interests: quality control; phytomedication; pharmaceutical forms; analytical techniques; thermogravimetry

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Guest Editor
Pharmaceutical Sciences Postgraduate Center for Biological and Health Sciences, State University of Paraíba, Av. Juvêncio Arruda, S/N, Campina Grande 58429-600, Paraíba, Brazil
Interests: drug delivery systems; hybrid materials; pharmaceutical technology; photodynamic therapy; drug discovery; antibacterial therapy
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Special Issue Information

Dear Colleagues,

Active compounds derived from natural products or synthesized compounds by planning and rational development make it possible to obtain medicines to treat a range of diseases. In this sense, prospecting or the synthesis of semi-synthetic or synthetic bioactive compounds, with the support of computational studies, provides the supply of different pharmaceutical assets from those existing on the market. In this sense, the advancement in the design of pharmaceutical forms (macro, micro, and nanostructure) allows the rescue and ensures the quality, effectiveness, and safety of the product.

Thus, the publication of expertise in this area will contribute to the production of new molecules that have adequate pharmacokinetic and pharmacodynamic properties, such as for the treatment of autoimmune diseases, neglected diseases, and those that still have no definite treatment. Therefore, in this Special Issue we will address aspects related to the prospecting of molecules in medicinal chemistry, pharmacological aspects, and pharmaceutical technological development.

Prof.Dr. Ana Claúdia D. Medeiros
Dr. João Augusto Oshiro Júnior
Guest Editors

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Keywords

  • active compounds
  • synthesis of biologically active molecules
  • pharmaceutical forms
  • nanosystems
  • quality control techniques
  • active pharmaceutical ingredients (APIs)
  • vegetable active pharmaceutical ingredients (VAPIs)

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Published Papers (3 papers)

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Research

16 pages, 1394 KiB  
Article
Anti-Tumor and Anti-Inflammatory Activity In Vivo of Apodanthera congestiflora Cogn. (Cucurbitaceae)
by Geovana F. G. Silvestre, Renally P. Lucena, Genil D. Oliveira, Helimarcos N. Pereira, Jhonatta A. B. Dias, Ivone A. Souza and Harley S. Alves
Pharmaceutics 2021, 13(5), 743; https://doi.org/10.3390/pharmaceutics13050743 - 18 May 2021
Cited by 5 | Viewed by 2577
Abstract
This work aimed to carry out a study of Apodanthera congestiflora by investigating its chemical composition and pharmacological potential. From the dichloromethane phase (Dic-Ac) of the A. congestiflora stems, three compounds were identified: cayaponoside C5b (Ac-1), cabenoside C (Ac-2) and fevicordin C [...] Read more.
This work aimed to carry out a study of Apodanthera congestiflora by investigating its chemical composition and pharmacological potential. From the dichloromethane phase (Dic-Ac) of the A. congestiflora stems, three compounds were identified: cayaponoside C5b (Ac-1), cabenoside C (Ac-2) and fevicordin C2 glucoside (Ac-3), being last identified for the first time as a natural product. These compounds were obtained by chromatographic methods and their structures were elucidated by means of spectroscopic analysis of IR, MS and NMR. In the quantification of Dic-Ac, it was possible to observe the presence of 7% of cayaponoside C5b. Dic-Ac showed significant toxicity for in vivo tests, with macroscopic and biochemical changes. The anti-inflammatory activity of Dic-Ac was investigated using the paw edema model. A decrease in inflammatory signs was observed in the first 5 h and the most effective dose in reducing edema with was 7.5 mg kg−1 (66.6%). Anti-tumor activity of Dic-Ac was evaluated by Ehrlich’s carcinoma model, which showed inhibition rate of 78.46% at 15 mg kg−1 dosage. The phytochemical investigation, together with the biological tests carried out in this study, demonstrated that A. congestiflora is a promising species in the search for therapeutics, since it contains substances with high pharmacological potential in its composition. Full article
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10 pages, 1123 KiB  
Article
Curcumin-Loaded Micelles Dispersed in Ureasil-Polyether Materials for a Novel Sustained-Release Formulation
by Kammila Martins Nicolau Costa, Mariana Rillo Sato, Tellys Lins Almeida Barbosa, Meiry Gláucia Freire Rodrigues, Ana Cláudia Dantas Medeiros, Bolívar Ponciano Goulart de Lima Damasceno and João Augusto Oshiro-Júnior
Pharmaceutics 2021, 13(5), 675; https://doi.org/10.3390/pharmaceutics13050675 - 8 May 2021
Cited by 14 | Viewed by 2798
Abstract
Vulvovaginal candidiasis (VVC) is a vulvar/vaginal infection that affects approximately 75% of women worldwide. The current treatment consists of antimicrobials with hepatotoxic properties and high drug interaction probabilities. Therefore, this study aimed to develop a new treatment to VVC based on micelles containing [...] Read more.
Vulvovaginal candidiasis (VVC) is a vulvar/vaginal infection that affects approximately 75% of women worldwide. The current treatment consists of antimicrobials with hepatotoxic properties and high drug interaction probabilities. Therefore, this study aimed to develop a new treatment to VVC based on micelles containing curcumin (CUR) dispersed in a ureasil-polyether (U-PEO) hybrid. The physical-chemical characterization was carried out in order to observe size, shape, crystallinity degree and particle dispersion in the formulation and was performed by dynamic light scattering (DLS), scanning electron microscopy (SEM), X-ray diffraction (XRD) and through in vitro release study. The results of DLS and SEM exhibited micelles with 35 nm, and encapsulation efficiency (EE) results demonstrated 100% of EE to CUR dispersed in the U-PEO, which was confirmed by the DRX. The release results showed that CUR loaded in U-PEO is 70% released after 10 days, which demonstrates the potential application of this material in different pharmaceutical forms (ovules and rings), and the possibility of multidose based on a single application, suggesting a higher rate of adherence. Full article
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16 pages, 3566 KiB  
Article
Seasonal Variations of Polyphenols Content, Sun Protection Factor and Antioxidant Activity of Two Lamiaceae Species
by Juliana de Medeiros Gomes, Márcio Vinícius Cahino Terto, Sócrates Golzio do Santos, Marcelo Sobral da Silva and Josean Fechine Tavares
Pharmaceutics 2021, 13(1), 110; https://doi.org/10.3390/pharmaceutics13010110 - 16 Jan 2021
Cited by 16 | Viewed by 3071
Abstract
Secondary metabolite production by plants is influenced by external environmental factors that can change depending on the seasons, which makes it important to know how the plant, through its metabolism, is able to adapt to these variations. Mentha x villosa and Plectranthus [...] Read more.
Secondary metabolite production by plants is influenced by external environmental factors that can change depending on the seasons, which makes it important to know how the plant, through its metabolism, is able to adapt to these variations. Mentha x villosa and Plectranthus amboinicus present in their chemical composition polyphenols, and through previous studies, it has been seen that these two species present promising in vitro photoprotective activity. The aim of this study was to evaluate seasonal alterations in photoprotective and antioxidant activities and the influence of factors such as precipitation levels and sun radiation incidence. Thus, polyphenol quantification, cromatographics (HPLC-DAD) and multivariate (PCA) analyses of extracts of the two species through twelve months were done. It was observed that the best months for photoprotective and antioxidant activities were September for M. villosa and July for P. amboinicus (SPF = 14.79). It was possible to conclude that solar radiation more clearly influences the production of phenolics and the increase of SPF in M. villosa, in addition to favoring the antioxidant activity of the two species, while precipitation seems to have no influence. Full article
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