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Updated: Sep 10, 2025

Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
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Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles

Published on: August 28, 2015

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PROTAC エナビリング・フォーミュレーションイン・ビボ:ポリメリック・キャリアEudragit EPOの影響

Nicole Hofmann1,2, Florian Johann1, Katharina Krollik1

  • 1Global Drug Product Development, Orals Development, the Healthcare Business of Merck KGaA, Frankfurter Straße 250, Darmstadt 64293, Germany.

Molecular pharmaceutics
|August 24, 2025
PubMed
まとめ

タンパク質分解を標的とするキメラ (PROTAC) のスプレー乾燥分散 (SDD) は,in vivoで不十分な曝露を示した. PROTACの溶解と安定化に影響を及ぼした,胆汁塩とリン酸の性能に依存した.

キーワード:
エウドラギットアモルフな固体の分散胆汁塩生物学的利用可能性配列を可能にするタンパク質分解を標的とするキメラ

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Drug Delivery: Overview01:16

Drug Delivery: Overview

The selection of a drug's delivery route depends upon its physicochemical properties, including lipid or water solubility and ionization, as well as the therapeutic requirement, such as immediate or sustained effect. These routes can be divided into three primary categories: enteral, parenteral, and topical.
Enteral delivery involves administering drugs directly through swallowing, sublingual placement, or buccal application. Orally administered drugs predominantly navigate the...
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Factors Influencing Drug Absorption: Pharmaceutical Parameters01:28

Factors Influencing Drug Absorption: Pharmaceutical Parameters

Solid dosage forms such as tablets and capsules undergo rigorous manufacturing processes to ensure stability and effectiveness. Their dissolution and absorption properties are influenced significantly by the choice of excipients (inactive ingredients that serve various roles in the formulation), and the methodology applied during production. The manufacturing parameters, such as compression force and granulation techniques, significantly affect dissolution rates. Elevated compression forces...
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Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry01:20

Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry

Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...
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Carrier-Mediated Transport01:06

Carrier-Mediated Transport

Carrier-mediated transport is a pivotal process in drug absorption, particularly for lipid-insoluble drugs, and encompasses facilitated diffusion and active transport. Facilitated diffusion allows drugs to move along their concentration gradient without energy expenditure, while active transport utilizes ATP to drive drug movement against this gradient.
Active transport involves two types of membrane-spanning transporters: uptake and efflux. Uptake transporters are expressed in the small...
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Drug Delivery: Enteral Route01:18

Drug Delivery: Enteral Route

The enteral drug administration involves three primary routes: oral, sublingual, and buccal. Oral ingestion is the most prevalent, safe, economical, and convenient method for drug administration. However, it has certain drawbacks, including limited absorption due to the drug's low water solubility or poor membrane permeability, possible emesis from GI mucosa irritation, destruction of drugs by digestive enzymes or low gastric pH, and irregular absorption along with food or other drugs.
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Drug Delivery: Parenteral Route01:29

Drug Delivery: Parenteral Route

The parenteral route is a critical method of drug administration. It delivers compounds directly into the systemic circulation and bypasses the gastrointestinal tract. This approach is particularly advantageous for drugs that exhibit poor absorption or instability when administered orally.
There are three primary parenteral routes: intravenous (IV), intramuscular (IM), and subcutaneous (SC). The IV route introduces the drug directly into the bloodstream, ensuring immediate action. The IM route...
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