小分子药物传递与製剂的创新

颠覆性技术为新产品发布带来成长机会

儘管小分子是适用于所有适应症的主要药物类别，但它们面临着威胁药物传递有效性的一些挑战。这些包括脱靶效应、生物有效性差、溶解度差、全身毒性和渗透性差。儘管小分子药物开发平臺仍然是主要的治疗药物类别，但加强研究和开发以改进药物传输方法至关重要。 Frost & Sullivan 对小分子药物递送最新趋势的分析涵盖了有机、无机和无载体小分子药物递送系统 (DDS) 的开发，以及提高患者依从性和靶向小分子递送的製剂开发。

小分子药物修饰方法，例如官能基修饰、遮罩不需要的化学基团和标靶配体缀合，是普及的药物传递方法。然而，还有其他方法可以修饰药物并实现所需的药物特性，即高溶解度和生物有效性、更好的标靶递送，例如前驱药物策略、小分子药物缀合物（SMDC）和多效价递送系统也正在出现。

随着用于新型 DDS 开发的先进技术平台的出现，新型小分子 DDS 正在得到更广泛的采用。脂质基、聚合物基和树状聚合物DDS 的发展正在加速。这些改善了小分子的缓释性和靶向特异性。例如，可以使用现有或新的递送系统的改进版本来特异性标靶化癌细胞。

新兴的智慧和可编程刺激响应递送系统是该行业的颠覆性技术，可以使用任何类型的载体来靶向和持续释放小分子药物。奈米载体和奈米製剂是针对多种适应症开发的所有类型的运载工具的主要行业趋势。胞外体和血液成分等天然来源的载体的生物相容性和生物分解性特性正在研究中。在口服製剂领域，脂质载体处于领先地位，特别是对于疏水性小分子。无载体、自组装奈米药物正成为下一代小分子药物。

这些新的发展和配方方法有助于提高患者的依从性。用于癌症和肺部疾病的干粉吸入製剂可提高小分子药物的生物有效性和患者依从性，特别是与注射剂相比。虽然口服和注射製剂仍然是癌症、神经系统和肺部疾病最广泛使用的给药方法之一，但舌下给药目前正在研究中。

目录

策略要务

• 为什么成长如此困难？
• 策略要务 8 (TM)：成长抑制因素
• The Strategic Imperative 8（TM）
• 关键策略要务对小分子药物输送产业发展的影响
• 成长机会推动Growth Pipeline Engine（TM）
• 调查方法

成长机会分析

• 促进因素
• 促生长因子分析
• 成长抑制因素
• 成长抑制因素分析
• 分析范围
• 分割
• 小分子药物传递的挑战

药物传输方法

• 小分子药物递送的趋势
• 小分子药物递送法简介
• 药物修饰方法以提高生物有效性
• 药物修饰方法的领先创新者
• 透过配体缀合改善标靶递送
• 主要创新者 - 配体缀合
• 职业
• 微脂体
• 脂质奈米粒子
• 尼奥体
• 新兴脂质有机载体的领先创新者
• 聚合物胶束
• 聚合物奈米颗粒
• 聚合物微球
• 聚合物载体领域的领先创新者
• 脂质/聚合物混合奈米粒子
• 水凝胶
• 树状聚合物
• 碳点
• DNA奈米机器人
• 新兴有机载体的主要创新者
• 天然载体
• 无机载体
• 无载体药物
• 新兴平台－可程式DDS
• 智慧刺激反应系统
• 奈米颗粒作为 DDS 的载体
• 人工智慧在选择药物传输载体和製剂中的作用

公式

• 小分子药物递送製剂系统
• 小分子给药方法和製剂
• 辅料在配方中的作用
• 吸入粉末配方
• 主要创新者
• 口服製剂中的 LNP
• 口服製剂和给药领域的主要创新者和创新
• 注射剂中的聚合物 DDS
• 主要创新者
• 口腔/舌下给药的发展
• 按疾病领域分類的小分子 DDS 趋势

市场动态

• 小分子药物输送产业参与者
• 小分子DDS合作现状
• 领先的 CDMO 公司为小分子递送提供先进的药物传递和配方平台

成长机会宇宙

• 成长机会1：透过与CDMO合作加强研发活动
• 成长机会 2：将人工智慧融入先进的药物输送方法
• 成长机会3：简单的给药方式提高病人依从性

附录

下一步

Disruptive Technologies Drive Growth Opportunities for New Product Launches

Small molecules, which are the leading drug class across indications, face several issues that threaten their drug delivery efficacy. They suffer from off-target effects, poor bioavailability, low solubility, systemic toxicity, and poor permeability. While the small molecule drug development pipeline remains a leading therapeutic class, it is essential to intensify R&D to improve drug delivery approaches. This Frost & Sullivan analysis of the latest advances in small molecule drug delivery covers developments in organic, inorganic, and carrier-free small molecule drug delivery systems (DDSs) as well as developments in formulations for improved patient adherence and targeted small molecule delivery.

Small molecule drug modification approaches-such as the modification of functional groups, masking undesirable chemical groups, conjugation of targeting ligands-remain a widespread method for drug delivery. However, other approaches are emerging, including prodrug strategies, small molecule-drug conjugates (SMDCs), and multivalent delivery systems, which serve to modify the drug and achieve desirable drug properties-higher solubility and bioavailability and better targeted delivery.

As advanced technology platforms for the development of novel DDSs emerge, new small molecule DDSs experience more widespread adoption. Development has accelerated for lipid-based, polymer-based, and dendrimer DDSs. These improve the sustained release and target specificity of small molecules. For instance, cancer cells are specifically targeted using improved versions of the existing delivery systems and newer delivery systems.

Emerging smart and programmable stimuli-response delivery systems are industry-disrupting technologies that can use any type of carrier for targeted and sustained small molecule drug release. Nanocarriers and nanoformulations are a key industry trend across all delivery vehicle types under development for multiple indications. Naturally derived carriers-such as exosomes and blood components-are under research for their biocompatibility and biodegradability properties. Lipid-based carriers lead in the oral formulations segment, especially for small hydrophobic molecules. Carrier-free self-assembly nanodrugs are emerging as the next generation of small molecule drugs.

These new developments and approaches in formulations help improve patient adherence. Dry powder inhalable formulations for cancer and pulmonary diseases increase the bioavailability of small molecule drugs and patient adherence, especially in comparison to injectables. Oral formulations and injectables remain one of the most widely adopted modes of administration for cancer and neurological and pulmonary diseases, while the sublingual mode is under exploration.

Table of Contents

Strategic Imperatives

• Why Is It Increasingly Difficult to Grow?The Strategic Imperative 8™: Factors Creating Pressure on Growth
• The Strategic Imperative 8™
• The Impact of the Top 3 Strategic Imperatives on Advances in the Small Molecule Drug Delivery Industry
• Growth Opportunities Fuel the Growth Pipeline Engine™
• Research Methodology

Growth Opportunity Analysis

• Growth Drivers
• Growth Driver Analysis
• Growth Restraints
• Growth Restraint Analysis
• Scope of Analysis
• Segmentation
• Challenges in Small Molecule Drug Delivery

Drug Delivery Approaches

• Trends in Small Molecule Drug Delivery
• Introduction to Small Molecule Drug Delivery Approaches
• Drug Modification Approaches That Enhance Bioavailability
• Key Innovators in Drug Modification Approaches
• Ligand Conjugation for an Improved Targeted Delivery
• Key Innovators - Ligand Conjugation
• Carriers
• Liposomes
• Lipid NPs
• Niosomes
• Key Innovators in Emerging Lipid-based Organic Carriers
• Polymeric Micelles
• Polymeric NPs
• Polymeric Microspheres
• Key Innovators in Polymer Based Carriers
• Lipid-polymer Hybrid NPs
• Hydrogels
• Dendrimers
• Carbon Dots
• DNA Nanobots
• Key Innovators in Emerging Organic Carriers
• Naturally Derived Carriers
• Inorganic Carriers
• Carrier-free Drugs
• Emerging Platforms-Programmable DDSs
• Smart Stimuli-response Systems
• Nanoparticles as Carriers for DDSs
• The Role of AI in Selecting Drug Delivery Vehicles and Formulations

Formulations

• Small Molecule Drug Delivery Formulation Systems
• Small Molecule Mode of Administration and Formulations
• The Role of Excipients in Formulation
• Inhalable Powder Formulations
• Key Innovators
• LNPs in Oral Formulations
• Key Innovators and Innovations in Oral Formulation and Delivery
• Polymeric DDSs in Injectables
• Key Innovators
• Developments in Buccal/Sublingual Delivery
• Small Molecule DDS Trends per Disease Area

Market Dynamics

• Small Molecule Drug Delivery Industry Players
• Collaboration Landscape for Small Molecule DDS
• Key CDMO Players Offering Advanced Drug Delivery and Formulation Platforms for Small Molecule Delivery
• Key CDMO Players Offering Advanced Drug Delivery and Formulation Platforms for Small Molecule Delivery
• Key CDMO Players Offering Advanced Drug Delivery and Formulation Platforms for Small Molecule Delivery

Growth Opportunity Universe

• Growth Opportunity 1: Collaborating with CDMOs to Intensify R&D Activities
• Growth Opportunity 2: Integrating AI for Advanced Drug Delivery Approaches
• Growth Opportunity 3: Simpler Administration Modes That Increase Patient Adherence

Appendix

• Technology Readiness Levels (TRL): Explanation

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