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Pharmaceuticals
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Polymorphs, Salts, Cocrystals and Cationic Lipid Nanoparticle Complexes in Drug...
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Polymorphs, Salts, Cocrystals and Cationic Lipid Nanoparticle Complexes in Drug Delivery

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Pharmaceutical Technology".

Deadline for manuscript submissions: closed (25 November 2024) | Viewed by 4642

Special Issue Editor

Prof. Dr. Stephen Robert Byrn

E-Mail Website
Guest Editor
Department of Industrial and Physical Pharmacy, School of Pharmacy and Pharmaceutical Sciences, Purdue University, 575 Stadium Mall Drive, West Lafayette, IN 47906, USA
Interests: solid state chemistry; pair distribution function; synchrotron X-ray diffraction; solid nanoparticles; drug quality; polymorphs; salts; cocrystals; amorphous forms

Special Issue Information

Dear Colleagues,

Polymorphs, salts, cocrystals, and solid lipid nanoparticles are key techniques for delivering ionic pharmaceuticals through oral and injectable forms. Co-processing drugs with one or more additional agents is also emerging as an effective strategy for drug delivery in these forms. Specifically, polymorphs created by melt crystallization, like Form III ritonavir, have shown potential in increasing blood levels and drug solubility. Similarly, forming salts in conventional crystals or with cationic lipids enhances drug delivery. Cocrystals use noncovalent forces and coformers to modify drug delivery, while co-processed systems, as exemplified by Zelboraf's new formulation, improve solubility and blood levels. This special issue will examine these strategies, highlighting how solid state chemistry can advance drug delivery.

Prof. Dr. Stephen Robert Byrn
Guest Editor

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Published Papers (3 papers)

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Research

16 pages, 6355 KiB  
Article
Solid-State NMR Characterization of Mefloquine Resinate Complexes Designed for Taste-Masking Pediatric Formulations
by Leandro B. Borré, Eduardo G. R. Sousa, Rosane A. S. San Gil, Mateus M. Baptista, Alexandre A. Leitão, João M. A. R. De Almeida, Olívia Carr, Osvaldo N. Oliveira, Jr., Flávio M. Shimizu and Thiago F. Guimarães
Pharmaceuticals 2024, 17(7), 870; https://doi.org/10.3390/ph17070870 - 2 Jul 2024
Viewed by 712
Abstract
Mefloquine (MQ) is an antimalarial medication prescribed to treat or malaria prevention.. When taken by children, vomiting usually occurs, and new doses of medication frequently need to be taken. So, developing pediatric medicines using taste-masked antimalarial drug complexes is mandatory for the success [...] Read more.
Mefloquine (MQ) is an antimalarial medication prescribed to treat or malaria prevention.. When taken by children, vomiting usually occurs, and new doses of medication frequently need to be taken. So, developing pediatric medicines using taste-masked antimalarial drug complexes is mandatory for the success of mefloquine administration. The hypothesis that binding mefloquine to an ion-exchange resin (R) could circumvent the drug’s bitter taste problem was proposed, and solid-state 13C cross-polarization magic angle spinning (CPMAS) NMR was able to follow MQ–R mixtures through chemical shift and relaxation measurements. The nature of MQ–R complex formation could then be determined. Impedimetric electronic tongue equipment also verified the resinate taste-masking efficiency in vitro. Variations in chemical shifts and structure dynamics measured by proton relaxation properties (e.g., T1ρH) were used as probes to follow the extension of mixing and specific interactions that would be present in MQ–R. A significant decrease in T1ρH values was observed for MQ carbons in MQ–R complexes, compared to the ones in MQ (from 100–200 ms in MQ to 20–50 ms in an MQ–R complex). The results evidenced that the cationic resin interacts strongly with mefloquine molecules in the formulation of a 1:1 ratio complex. Thus, 13C CPMAS NMR allowed the confirmation of the presence of a binding between mefloquine and polacrilin in the MQ–R formulation studied. Full article
(This article belongs to the Special Issue Polymorphs, Salts, Cocrystals and Cationic Lipid Nanoparticle Complexes in Drug Delivery)
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16 pages, 4834 KiB  
Article
Improving the Dissolution Rate and Bioavailability of Curcumin via Co-Crystallization
by Hao Wang, Chenxuan Zheng, Fanyu Tian, Ziyao Xiao, Zhixiong Sun, Liye Lu, Wenjuan Dai, Qi Zhang and Xuefeng Mei
Pharmaceuticals 2024, 17(4), 489; https://doi.org/10.3390/ph17040489 - 11 Apr 2024
Cited by 3 | Viewed by 1940
Abstract
Curcumin (CUR) is a natural polyphenolic compound with various pharmacological activities. Low water solubility and bioavailability limit its clinical application. In this work, to improve the bioavailability of CUR, we prepared a new co-crystal of curcumin and L-carnitine (CUR-L-CN) via liquid-assisted grinding. Both [...] Read more.
Curcumin (CUR) is a natural polyphenolic compound with various pharmacological activities. Low water solubility and bioavailability limit its clinical application. In this work, to improve the bioavailability of CUR, we prepared a new co-crystal of curcumin and L-carnitine (CUR-L-CN) via liquid-assisted grinding. Both CUR and L-CN have high safe dosages and have a wide range of applications in liver protection and animal nutrition. The co-crystal was fully characterized and the crystal structure was disclosed. Dissolution experiments were conducted in simulated gastric fluids (SGF) and simulated intestinal fluids (SIF). CUR-L-CN exhibited significantly faster dissolution rates than those of pure CUR. Hirshfeld surface analysis and wettability testing indicate that CUR-L-CN has a higher affinity for water and thus exhibits faster dissolution rates. Pharmacokinetic studies were performed in rats and the results showed that compared to pure CUR, CUR-L-CN exhibited 6.3-times-higher AUC0–t and 10.7-times-higher Cmax. Full article
(This article belongs to the Special Issue Polymorphs, Salts, Cocrystals and Cationic Lipid Nanoparticle Complexes in Drug Delivery)
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16 pages, 2156 KiB  
Article
Potency and Powder X-ray Diffraction (PXRD) Evaluation of Levothyroxine Sodium Tablets under Ambient, Accelerated, and Stressed Conditions
by Mercy A. Okezue, Stephen R. Byrn, Josiah Probost, Madison Lucas and Kari L. Clase
Pharmaceuticals 2024, 17(1), 42; https://doi.org/10.3390/ph17010042 - 27 Dec 2023
Viewed by 1545
Abstract
Levothyroxine tablets, although highly prescribed in the United States, have been one of the most frequently recalled products. Because of the importance of the medication, several efforts have been put in place by the United States Food and Drug Administration (US FDA) to [...] Read more.
Levothyroxine tablets, although highly prescribed in the United States, have been one of the most frequently recalled products. Because of the importance of the medication, several efforts have been put in place by the United States Food and Drug Administration (US FDA) to control the quality of levothyroxine tablets available to patients using the drug. The choice of excipients used in the formulation has been shown to impact the hygroscopicity and microenvironment, and ultimately the stability of the levothyroxine tablets formulations. Based on information generated from the US FDA Enforcement Report database, one of the main reasons for recalls is the low potency of different batches of the product. The yearly product recall trends for levothyroxine formulations were determined using the FDA Enforcement Report database. Three brands of levothyroxine tablets were selected with excipient lists similar to those products that have been historically recalled. The samples were placed at ambient (~23 °C), accelerated stability (40 °C/75% RH), and stress (50 °C/75% RH) conditions for up to 6 months. Sample potencies were determined at 0, 1.5, 3, and 6 months using the methods for assay and impurities in the United States Pharmacopeia (USP) monograph for levothyroxine tablets. Additional sample monitoring was conducted by overlaying the initial powder X-ray diffractograms (PXRD) of the samples from 0 months with the patterns generated thereafter. There has been a decline in the number of levothyroxine tablets recalled over the years. The highest numbers of recalls were recorded in the years 2013 [33] and 2020 [23]; no recalls occurred in the years 2019 and 2022. All of the brands evaluated met the USP 95.0–105.0% assay requirements at 1.5 months under accelerated conditions; only one of the brands complied at 3 months. Under ambient conditions, two brands were stable at 6 months, with borderline assay results. For stability, levothyroxine was found in microgram quantities in the formulations and PXRD could not detect changes at these low levels. However, we found some distinguishing data for samples under stress conditions. Full article
(This article belongs to the Special Issue Polymorphs, Salts, Cocrystals and Cationic Lipid Nanoparticle Complexes in Drug Delivery)
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