Oral Bioavailability and Drug Delivery From Basics to Advanced Concepts and Applications

Improve the performance and viability of newly-developed and approved drugs with this crucial guide

Bioavailability is the parameter which measures the rate and extent to which a drug reaches a user’s circulatory system depending on the method of administration. For example, intravenous administration produces a bioavailability of 100%, since the drugs are injected directly into the circulatory system; in the case of oral administration, however, bioavailability can vary widely based on factors which, if not properly understood, can result in a failure in drug development, adverse effects, and other complications. The mechanics of oral bioavailability are therefore critical aspects of drug development.

Oral Bioavailability and Drug Delivery provides a comprehensive introduction to this subject as well as its drug development applications. Beginning with foundations and basic terminology, it provides a thorough understanding of the challenges and barriers to oral bioavailability as well as the possibilities for improving this parameter. The result is an indispensable tool for drug development research.

Oral Bioavailability and Drug Delivery readers will also find:

• Discussion questions in many chapters to facilitate comprehension
• Detailed discussion of topics including dissolution, absorption, metabolism, and more
• Real-world examples of methods in actions throughout

Oral Bioavailability and Drug Delivery is ideal for pharmaceutical scientists working in drug discovery and development; researchers in chemistry, biology, pharmacology, and other related fields; and graduate courses in drug development and delivery.

Ming Hu, PhD, is Professor of Pharmaceutics at the College of Pharmacy, University of Houston, Texas, USA.

Xiaoling Li, PhD, is Professor of Pharmaceutics at the TJL School of Pharmacy, University of the Pacific, California, USA.

1 Barriers to Oral Bioavailability-An Overview

2 Solubility of Pharmaceutical Solids 

3 In Vitro Dissolution of Pharmaceutical Solids  

4 Biological and Physiological Features of Gastrointestinal Tract Relevant to Oral Drug Absorption

5 Absorption of Drugs via Passive Diffusion and Carrier-Mediated Pathways

6 Determinant Factors for Passive Absorption of Drugs

7 Protein Binding and Drug Distribution 

8 Drug Transport across the Placental Barrier 

9 Biopharmaceutics Classification Systems: Theory and Practice 

10 Effects of Food on Drug Absorption

11 Drug Metabolism in Gastrointestinal Tract

12 Liver Drug Metabolism

13 Urinary Excretion of Drugs and Drug Reabsorption

14 Excretion of Drugs and Their Metabolites in Bile

15 Pharmacokinetic Behaviors of Orally Administered Drugs

16 In Vitro-In Vivo Correlation of Pharmaceutical Dosage Forms

17 Advanced Concepts in Oral Bioavailability Research-An Overview

18 Expression and Pharmaceutical Relevance of Intestinal Transporters  

19 Amino Acid Drug Transporters

20 Drug Transporters and Their Role in Absorption and Disposition of Peptides and Peptide Based Pharmaceuticals

21 OATP Transporters in Hepatic and Intestinal Uptake of Orally Administered Drugs 

22 ABC Transporters in Intestinal and Liver Efflux

23 Interplay between metabolic enzymes and efflux transporters

24 Systemic versus Local Bioavailability enabled by Enterohepatic Recycling 

25 Intestinal Microbiome and Its Impact on Metabolism and Safety of Drugs 

26 Drug-Drug Interactions and Drug-Dietary Chemical Interactions

27 Regulatory Considerations in Metabolism- and Transport-Based Drug Interactions 

28 Formulation approaches to improve oral bioavailability of drugs

29 Lipid Based and Self Emulsified Oral Drug Delivery Systems

30 Oral Delivery of Nanoparticles: Challenges and Opportunities 

31 Oral delivery of Therapeutic Peptides: Strategies for product development

32 Prodrugs to Improve Oral Delivery

33 Gastroretentive Drug Delivery Systems

34 Enhancement of Oral Bioavailability using 3D printing Technologies

35 Anatomical and Physiological Factors Affecting Oral Drug Bioavailability in Rats, Dogs, Monkeys and Humans

36 In vivo Methods for Determining Oral Bioavailability

37 Caco-2 Cell Culture Model for Oral Drug Absorption

38 OATP Overexpressed cells and their use in drug uptake studies 

39 Use of Human Intestinal and Hepatic Tissue Fractions and Microbiome as Models in Assessment of Drug Metabolism and its Impact on Oral Bioavailability 

40 Liver Perfusion and Primary Hepatocytes for Studying Drug Metabolism and Metabolite Excretion

41 Determination of Regulation of Drug Metabolizing Enzymes and Transporters  

42 Intestinal Perfusion Methods for Oral Drug Absorptions

43 In Silico Prediction of Oral Drug Absorption

44 Computational Modeling of Drug Oral Bioavailability  

45 Blood-Brain Barrier Permeability Assessment for Small Molecule Drug Discovery Using Computational Techniques

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