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Drug Formulation: Solubilization and Controlled-Release Strategies

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Dear Colleagues,

The processes of solubilization and controlled release of poorly water-soluble drugs are of critical importance in the pre-formulation phase of pharmaceutical development.

In recent years, a considerable number of new drug candidates have been industrialized, with nearly 70% of them exhibiting low water solubility. This characteristic significantly limits their dissolution rate and, consequently, their bioavailability. This undoubtedly represents a major challenge for the pharmaceutical industry. The discovery and development of new technological tools for drug solubilization—tools that preserve the physicochemical and therapeutic properties of active compounds—would therefore represent a significant scientific and industrial achievement.

From a pharmacological perspective, advancing our understanding of the mechanisms of interaction and functional properties of controlled drug release systems has also become a key priority in drug formulation. These systems are essential for optimizing therapeutic efficacy by delivering the appropriate amount of an active ingredient at the right time and to the precise site of action.

This Special Issue is dedicated to the latest advances in solubilization and controlled-release strategies for poorly water-soluble drugs. It aims to compile research and review papers on innovative topics including advanced solubilization techniques (e.g., nanocrystals, DES), controlled-release systems (stimuli-responsive, 3D-printed), emerging materials (MOFs, graphene), targeted delivery (exosomes, BBB penetration), green chemistry, AI-driven formulations, oral/non-oral delivery solutions, regulatory considerations, combination therapies, and applications for specific populations. We invite authors to submit original research articles and comprehensive reviews addressing innovative solubilization approaches, novel controlled-release technologies, and tailored pharmaceutical forms designed to meet the needs of specific patient populations and pathologies. Special attention should also be given to the route of administration, ensuring the highest possible standards of drug efficacy and safety.

Prof. Dr. María Peña Fernández
Guest Editor

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21 pages, 1921 KB

Open AccessArticle

Liposomal Formulations for Efficient Delivery of a Novel, Highly Potent Pyrimidine-Based Anticancer Drug

by Sofia Teixeira, Débora Ferreira, Ana Rita O. Rodrigues, Ligia R. Rodrigues, Elisabete M. S. Castanheira and Maria Alice Carvalho

Pharmaceuticals 2025, 18(8), 1210; https://doi.org/10.3390/ph18081210 - 15 Aug 2025

Viewed by 497

Abstract

Background/Objectives: Cancer is one of the deadliest diseases worldwide. Despite the existing treatments, the adverse side effects and the increasing drug resistance to the current therapies lead to a reduced quality of life for patients and poor prognosis. The pyrimido[5,4-d]pyrimidine compound (PP) was identified as a promising new anticancer drug due to its potent activity against colorectal and triple-negative breast cancers; however it showed poor aqueous solubility and safety profile. This study aimed the synthesis of compound PP, its encapsulation in liposomal formulations based on phosphatidylcholines (PC), the characterization of liposomal formulations and its biological evaluation. Methods: A new synthesis method for PP was developed. The compound was incorporated into different liposomal formulations. The hydrodynamic size, polydispersity, and zeta potential of loaded and non-loaded formulations were measured by DLS. The cytotoxic effects of compound PP, placebo nanoformulations, and PP-loaded nanoformulations were assessed in colorectal (HCT 116) and triple-negative breast cancer (MDA-MB-231) cell lines, as well as in non-tumor BJ-5ta cells. Results: The PP compound was efficiently synthesized. The PP-loaded liposomal formulations exhibit sizes below 150 nm, low polydispersity, and long-time stability upon storage at 4 °C. The antitumor compound was encapsulated with excellent efficiency, and sustained release profiles were obtained. The PP compound showed high activity against HCT 116 (IC₅₀ = 2.04 ± 0.45 µM) and MDA-MB-231 (IC₅₀ = 5.24 ± 0.24 µM) cell lines. DPPC-containing formulations were effective against cancer cells, but showed toxicity comparable to free PP in BJ-5ta normal cells. Conversely, PP-EggPC-Chol-L formulation displayed strong anticancer activity with residual toxicity to normal cells. Conclusions: The PP-loaded liposomal formulation, composed of 70% PC from egg yolk (EggPC) and 30% cholesterol (Chol), designated as PP-EggPC-Chol-L, was the most promising formulation, showing effective anticancer activity in both cancer cell lines and a significant improvement in the safety profile which is of utmost importance to progress to the next phase of drug development. Full article

(This article belongs to the Special Issue Drug Formulation: Solubilization and Controlled-Release Strategies)

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