Introduction to Biopharmaceutics and its Role in Drug Development

Barbour, Nancy P.; Lipper, Robert A.

doi:10.1007/978-0-387-72379-2_1

Cited by 5 publications

(3 citation statements)

References 59 publications

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“…Compared to B1 , the peptoid D2 has a reduced number of hydrogen donors due to the peptoid backbone, higher hydrophilicity (featuring five positive charges, see Figure 1 ) and a higher degree of rotational flexibility. Rotational flexibility [ 58 ] is generally directly proportional to molecular weight, and it counts non-ring bonds to nonterminal non-hydrogen atoms. Despite the promising results, toxicity needs to be further assessed, e.g., by cytotoxicity to fibroblasts or other skin cells, as well as in vivo.…”

Section: Discussionmentioning

confidence: 99%

In Vitro ADME Properties of Two Novel Antimicrobial Peptoid-Based Compounds as Potential Agents against Canine Pyoderma

et al. 2018

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Antimicrobial peptides (AMPs) hold promise as the next generation of antimicrobial agents, but often suffer from rapid degradation in vivo. Modifying AMPs with non-proteinogenic residues such as peptoids (oligomers of N-alkylglycines) provides the potential to improve stability. We have identified two novel peptoid-based compounds, B1 and D2, which are effective against the canine skin pathogen Staphylococcus pseudintermedius, the main cause of antibiotic use in companion animals. We report on their potential to treat infections topically by characterizing their release from formulation and in vitro ADME properties. In vitro ADME assays included skin penetration profiles, stability to proteases and liver microsomes, and plasma protein binding. Both B1 and D2 were resistant to proteases and >98% bound to plasma proteins. While half-lives in liver microsomes for both were >2 h, peptoid D2 showed higher stability to plasma proteases than the peptide-peptoid hybrid B1 (>2 versus 0.5 h). Both compounds were suitable for administration in an oil-in-water cream formulation (50% release in 8 h), and displayed no skin permeation, in the absence or presence of skin permeability modifiers. Our results indicate that these peptoid-based drugs may be suitable as antimicrobials for local treatment of canine superficial pyoderma and that they can overcome the inherent limitations of stability encountered in peptides.

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Section: Discussionmentioning

confidence: 99%

In Vitro ADME Properties of Two Novel Antimicrobial Peptoid-Based Compounds as Potential Agents against Canine Pyoderma

et al. 2018

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“…For example, on apical membrane, efflux transporters prevent the entry of undesirable, potentially toxic materials into the systemic circulation. [10] Transporters are categorized into two super families: ATP-binding cassette (ABC) transporters and Solute carrier (SLC) transporters.…”

Section: Intestinal Transportersmentioning

confidence: 99%

Influence of excipients on drug absorption via modulation of intestinal transporters activity

Thakkar¹,

Desai²

2015

Asian J Pharm

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O ne of the major factors affecting oral drug bioavailability is the activity of intestinal transport proteins, particularly for the drugs that undergo absorption by active transport mechanism. Many of the active pharmacological agents and the excipients used in their formulation are reported to modulate the activity of these transporters thereby either enhancing or decreasing the drug absorption and its systemic availability. These excipients are considered pharmacologically "inert" and have been used since years in pharmaceutical formulations. Appreciable interest is developing on the data demonstrating the role of excipients in altering the drug absorption across the intestine. Careful selection of the excipients thus is very important. A correctly chosen excipient can enhance the drug bioavailability and thus its therapeutic efficacy without increasing its dose. For locally acting drugs having systemic side effects, a proper excipient could lead to a decrease in its systemic absorption, thus reducing its side effects. This review focuses on the current findings of the excipients identified to modulate the activity of transporters, their mechanism of modulating the transporter's activity and various formulation strategies using these excipients to enhance drug absorption.

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“…" Definition Biopharmaceutics: Barbour and Lipper (2008) have noted that, by introducing the prefix bio to the word pharmaceutics, it follows that biopharmaceutics study the interdependence of biological aspects of the living organism (i.e., the patient) and the physical/chemical principles that govern the preparation and behavior of the medicinal agent and/or the drug product (Barbour and Lipper 2008). The discipline examines the interrelationship of the physical/chemical properties of the drug, the dosage form in which the drug is delivered, and the route of administration, on the rate and extent of systemic drug absorption (Shargel et al 2012).…”

mentioning

confidence: 99%