Pharmaceutical approaches for enhancing solubility and oral bioavailability of poorly soluble drugs

Nyamba, Isaïe; Sombié, Charles B; Yabré, Moussa; Zimé-Diawara, Hermine; Yaméogo, Josias; Ouédraogo, Salfo; Lechanteur, Anna; Semdé, Rasmané; Evrard, Brigitte

doi:10.1016/j.ejpb.2024.114513

European Journal of Pharmaceutics and Biopharmaceutics

2024

DOI: 10.1016/j.ejpb.2024.114513

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Pharmaceutical approaches for enhancing solubility and oral bioavailability of poorly soluble drugs

Isaïe Nyamba,

Charles B Sombié,

Moussa Yabré

et al.

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2024

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Cited by 4 publications

References 166 publications

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Metal Oxide Nanoparticles as Efficient Nanocarriers for Targeted Cancer Therapy: Addressing Chemotherapy-Induced Disabilities

Yassin,

Al-Otibi,

Al-Sahli

et al. 2024

Cancers

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Cancer remains a predominant global health concern, necessitating effective treatment options. Conventional cancer therapies, particularly chemotherapy, often face constraints such as low selectivity, insufficient solubility, and multidrug resistance (MDR), which diminish effectiveness and exacerbate negative effects. Metal oxide nanoparticles (MONPs), such as iron oxide, zinc oxide, and copper oxide, offer a promising solution by enhancing targeted drug delivery, reducing systemic toxicity, and mitigating chemotherapy-induced disabilities like neurotoxicity and cardiotoxicity. Nanocarriers conjugated with drugs can improve drug delivery within the body and enhance their circulation in the bloodstream. Recent advancements in MONP synthesis and functionalization have further improved their stability and drug-loading capacity, making them a valuable tool in cancer treatment. MONPs have distinctive physicochemical characteristics, enabling better imaging, drug encapsulation, and targeted medication delivery to cancerous cells. These nanocarriers enhance treatment effectiveness through focused and controlled drug release, reducing off-target effects and addressing drug resistance. This review aims to explore the potential of MONPs as efficient nanocarriers for anticancer drugs, addressing limitations of traditional chemotherapy such as poor specificity, systemic toxicity, and drug resistance. Additionally, the review discusses recent advancements in MONP synthesis and functionalization, which enhance their stability, drug-loading capacity, and compatibility.

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Metal Oxide Nanoparticles as Efficient Nanocarriers for Targeted Cancer Therapy: Addressing Chemotherapy-Induced Disabilities

Yassin,

Al-Otibi,

Al-Sahli

et al. 2024

Cancers

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Overcoming Challenges in Small-Molecule Drug Bioavailability: A Review of Key Factors and Approaches

Wu,

Kwon,

Zhou

et al. 2024

IJMS

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The bioavailability of small-molecule drugs remains a critical challenge in pharmaceutical development, significantly impacting therapeutic efficacy and commercial viability. This review synthesizes recent advances in understanding and overcoming bioavailability limitations, focusing on key physicochemical and biological factors influencing drug absorption and distribution. We examine cutting-edge strategies for enhancing bioavailability, including innovative formulation approaches, rational structural modifications, and the application of artificial intelligence in drug design. The integration of nanotechnology, 3D printing, and stimuli-responsive delivery systems are highlighted as promising avenues for improving drug delivery. We discuss the importance of a holistic, multidisciplinary approach to bioavailability optimization, emphasizing early-stage consideration of ADME properties and the need for patient-centric design. This review also explores emerging technologies such as CRISPR-Cas9-mediated personalization and microbiome modulation for tailored bioavailability enhancement. Finally, we outline future research directions, including advanced predictive modeling, overcoming biological barriers, and addressing the challenges of emerging therapeutic modalities. By elucidating the complex interplay of factors affecting bioavailability, this review aims to guide future efforts in developing more effective and accessible small-molecule therapeutics.

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Dry Amorphization of Itraconazole Using Mesoporous Silica and Twin-Screw Technology

Richter,

Welzmiller,

Monsuur

et al. 2024

Pharmaceutics

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Background/Objectives: Amorphization of an active pharmaceutical ingredient (API) can improve its dissolution and enhance bioavailability. Avoiding solvents for drug amorphization is beneficial due to environmental issues and potential solvent residues in the final product. Methods: Dry amorphization using a twin-screw extruder is presented in this paper. A blend of mesoporous silica particles and crystalline itraconazole was processed using a pharma-grade laboratory scale twin-screw extruder. The influence of different screw configurations and process parameters was tested. Particle size and shape are compared in scanning electron microscopy (SEM) images. Differential scanning calorimetry (DSC) and X-ray diffraction (XRD) are used to determine the residual amount of crystalline itraconazole in the final product. Results: An optimized screw configuration for the process was found which leads to more than 90% amorphous API when processed at room temperature. Full amorphization was reached at 70 °C. The specific mechanic energy (SME) introduced into the material during twin-screw processing is crucial for the dry amorphization. The higher the SME, the lower the residual amount of crystalline API. Two months after processing, however, recrystallization was observed by XRD. Conclusions: Dry processing using a twin-screw extruder is continuous, free of solvents and can be performed at low temperatures. This study proves the concept of twin-screw processing with mesoporous silica for dry amorphization of itraconazole.

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Pharmaceutical approaches for enhancing solubility and oral bioavailability of poorly soluble drugs

Cited by 4 publications

References 166 publications

Metal Oxide Nanoparticles as Efficient Nanocarriers for Targeted Cancer Therapy: Addressing Chemotherapy-Induced Disabilities

Metal Oxide Nanoparticles as Efficient Nanocarriers for Targeted Cancer Therapy: Addressing Chemotherapy-Induced Disabilities

Overcoming Challenges in Small-Molecule Drug Bioavailability: A Review of Key Factors and Approaches

Dry Amorphization of Itraconazole Using Mesoporous Silica and Twin-Screw Technology

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