H2020Индивидуална стипендия2019–2021

OMECRY · Organic Mesocrystals: Formation and controlling of oriented nanoparticles of molecular solids for drug development

„Хоризонт 2020“ — Действия „Мария Склодовска-Кюри“

Период: 2019-10-01 → 2021-11-30
Финансиране от ЕС: 202 681 €
Участници: 1
Схема: MSCA-IF-EF-ST

Линиите свързват координатора с партньорите.

Накратко на български

Органичните мезокристали, създадени от подредени наночастици, се изследват чрез пример с ибупрофен. Те помагат за по-бързото разтваряне на лекарства, които трудно се абсорбират от организма поради ниска разтворимост във вода.

Този кратък обзор е генериран от изкуствен интелект

Кратко обяснение, генерирано от езиков модел по текста на CORDIS. Оригиналът е по-долу.

Резултати накратко

Organic Mesocrystals: Formation and controlling of oriented nanoparticles of molecular solids for drug development

Low aqueous solubility restricts the oral use of almost 90 % of new drug substances and even 40 % of drugs with market approval show poor solubility. A new approach to disintegrate the drug particles rapidly in an aqueous solution is highly requisite. Mesocrystals are self-assembled and crystallographically oriented attachments of nanoparticles formed via non-classical crystallization (NCC). The mesocrystals internal and external features such as voids, nanoparticles building units, crystallographic orientation, micron-size particles, and reactive surfaces will enable this drug for high dissolution. Therefore, the overall objective of this project has been to prepare low aqueous soluble drug in the form of mesocrystals and test their dissolution rate. Since the mesocrystals word was coined less than two decades ago, this formation process needs still better understanding to unveil the nucleation and growth of crystals. Investigating the formation of nucleus and growth shed light on to further understand the mechanism of NCC. Therefore, the in-situ characterizations of their different crystallization pathways in NCC were also included in this objective. The ibuprofen was chosen as model compound since this solubility is low as about 21 mg/L at 25 °C. Based on experimental methods and in situ studies, this action concludes that the high supersaturation with dispersed particles at the initial stage of crystallization and suitable additives are required to form ibuprofen mesocrystals. The experimental observation of liquid-liquid phase separation was apparent in pharmaceutical solids with low melting point and in situ studies confirmed that the dense liquid phase is not amorphous, and their molecular interactions are different than dimer of ibuprofen due to closely packed molecular environment. The dissolution of ibuprofen mesocrystals has enhanced compared with their classical grown single crystals.

Текст от CORDIS, на английски · Данни: CORDIS, © Европейски съюз

Цел на проекта

The OMECRY research action aims to enhance the dissolution of pharmaceutical solids in the form of mesocrystals, i.e. to promote the drug development. I will also investigate the formation mechanisms of the organic mesocrystals, and influence of the different additives on these processes. The low dissolution rate and poor aqueous solubility of emerging new drug candidates limit the formulation approaches, clinical application, and marketability in pharmaceutical industry. The preparation of active pharmaceutical ingredients (APIs) in the form of mesocrystals can enhance the dissolution rate suitable for drug delivery. The voids between highly oriented nanocrystals and high surface area of hierarchical structure in the non-classical pathway of mesocrystals formation play a role in the process. Different additives can be used to control the self-assembly of particles so that avoiding mesocrystals fusion into single crystals. A suitable additive can be screened through density functional theory calculations. The microstructure of mesocrystals and its transformation and particle growth can be investigated through time-dependent experiments using SEM, TEM and laser diffraction particle size analyser. Computed Tomography will be used for the first time to obtain the density mapping of mesocrystals surface in phase contrast mode. The dissolution rates and solubility of the mesocrystals are characterized and compared to its single crystals. The feasibility of drug dissolution will be investigated through in vitro studies. Although many inorganic mesocrystals has prepared for photocatalysis, energy storage applications, formation APIs in mesocrystals is a new strategy which provides insights that are needed for further understanding of mesocrystals formations thereby improve its applications especially for drug development.

Оригинален текст от CORDIS (на английски).

Участници

AALTO KORKEAKOULUSAATIO SR · EspooКоординаторФинландия