小分子藥物傳遞與製劑的創新

顛覆性技術為新產品發布帶來成長機會

儘管小分子是適用於所有適應症的主要藥物類別，但它們面臨著威脅藥物傳遞有效性的一些挑戰。這些包括脫靶效應、生物有效性差、溶解度差、全身毒性和滲透性差。儘管小分子藥物開發平臺仍然是主要的治療藥物類別，但加強研究和開發以改進藥物傳輸方法至關重要。 Frost & Sullivan 對小分子藥物遞送最新趨勢的分析涵蓋了有機、無機和無載體小分子藥物遞送系統 (DDS) 的開發，以及提高患者依從性和靶向小分子遞送的製劑開發。

小分子藥物修飾方法，例如官能基修飾、遮罩不需要的化學基團和標靶配體綴合，是普及的藥物傳遞方法。然而，還有其他方法可以修飾藥物並實現所需的藥物特性，即高溶解度和生物有效性、更好的標靶遞送，例如前驅藥物策略、小分子藥物綴合物（SMDC）和多效價遞送系統也正在出現。

隨著用於新型 DDS 開發的先進技術平台的出現，新型小分子 DDS 正在得到更廣泛的採用。脂質基、聚合物基和樹狀聚合物DDS 的發展正在加速。這些改善了小分子的緩釋性和靶向特異性。例如，可以使用現有或新的遞送系統的改進版本來特異性標靶化癌細胞。

新興的智慧和可編程刺激響應遞送系統是該行業的顛覆性技術，可以使用任何類型的載體來靶向和持續釋放小分子藥物。奈米載體和奈米製劑是針對多種適應症開發的所有類型的運載工具的主要行業趨勢。胞外體和血液成分等天然來源的載體的生物相容性和生物分解性特性正在研究中。在口服製劑領域，脂質載體處於領先地位，特別是對於疏水性小分子。無載體、自組裝奈米藥物正成為下一代小分子藥物。

這些新的發展和配方方法有助於提高患者的依從性。用於癌症和肺部疾病的乾粉吸入製劑可提高小分子藥物的生物有效性和患者依從性，特別是與注射劑相比。雖然口服和注射製劑仍然是癌症、神經系統和肺部疾病最廣泛使用的給藥方法之一，但舌下給藥目前正在研究中。

目錄

策略要務

• 為什麼成長如此困難？
• 策略要務 8 (TM)：成長抑制因素
• The Strategic Imperative 8（TM）
• 關鍵策略要務對小分子藥物輸送產業發展的影響
• 成長機會推動Growth Pipeline Engine（TM）
• 調查方法

成長機會分析

• 促進因素
• 促生長因子分析
• 成長抑制因素
• 成長抑制因素分析
• 分析範圍
• 分割
• 小分子藥物傳遞的挑戰

藥物傳輸方法

• 小分子藥物遞送的趨勢
• 小分子藥物遞送法簡介
• 藥物修飾方法以提高生物有效性
• 藥物修飾方法的領先創新者
• 透過配體綴合改善標靶遞送
• 主要創新者 - 配體綴合
• 職業
• 微脂體
• 脂質奈米粒子
• 尼奧體
• 新興脂質有機載體的領先創新者
• 聚合物膠束
• 聚合物奈米顆粒
• 聚合物微球
• 聚合物載體領域的領先創新者
• 脂質/聚合物混合奈米粒子
• 水凝膠
• 樹狀聚合物
• 碳點
• DNA奈米機器人
• 新興有機載體的主要創新者
• 天然載體
• 無機載體
• 無載體藥物
• 新興平台－可程式DDS
• 智慧刺激反應系統
• 奈米顆粒作為 DDS 的載體
• 人工智慧在選擇藥物傳輸載體和製劑中的作用

公式

• 小分子藥物遞送製劑系統
• 小分子給藥方法和製劑
• 輔料在配方中的作用
• 吸入粉末配方
• 主要創新者
• 口服製劑中的 LNP
• 口服製劑和給藥領域的主要創新者和創新
• 注射劑中的聚合物 DDS
• 主要創新者
• 口腔/舌下給藥的發展
• 按疾病領域分類的小分子 DDS 趨勢

市場動態

• 小分子藥物輸送產業參與者
• 小分子DDS合作現狀
• 領先的 CDMO 公司為小分子遞送提供先進的藥物傳遞和配方平台

成長機會宇宙

• 成長機會1：透過與CDMO合作加強研發活動
• 成長機會 2：將人工智慧融入先進的藥物輸送方法
• 成長機會3：簡單的給藥方式提高病人依從性

附錄

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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