Peptide Prodrugs for the Treatment of CNS Disorders: A Perspective for New Drugs

Chin, Chung Man; Chiba, Diego Eidy; Machado, Marcella Gabrielle Mendes; Vizioli, Ednir de Oliveira; Santos, Jean Leandro dos

doi:10.2174/0929867321666140217125526

Cited by 1 publication

(1 citation statement)

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“…For orally administered drug products, the active ingredient has to have sufficient permeability to be absorbed to achieve the desired therapeutic efficacy, including overcoming the Bblood-brain barrier^(BBB) for central nervous system therapies (65,83,(90)(91)(92). Many drugs of a highly polar nature or charged at physiological pH typically have very low permeabilities, such as carboxylic acids, strongly basic compounds such as amidines and guanidines, nucleosides, and nucleotides.…”

Section: Prodrugsmentioning

confidence: 99%

Drug Delivery Approaches in Addressing Clinical Pharmacology-Related Issues: Opportunities and Challenges

Wen¹,

Jung²,

2015

AAPS J

442

189

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Abstract. Various drug delivery approaches can be used to maximize therapeutic efficacy and minimize side effects, by impacting absorption, distribution, metabolism, and elimination (ADME) of a drug compound. For those drugs with poor water solubility or low permeability, techniques such as amorphous solid dispersion, liposomes, and complexations have been used to improve their oral bioavailability. Modified release (MR) formulations have been widely used to improve patient compliance, as well as to reduce side effects, especially for those drugs with short half-lives or narrow therapeutic windows. More than ten drugs using sterile long-acting release (LAR) formulations with clear clinical benefit have been successfully marketed. Furthermore, drug delivery systems have been used in delaying drug clearance processes. Additionally, modifying the in vivo drug distribution using targeted delivery systems has significantly improved oncology treatments. All the drug delivery approaches have their advantages and limitations. For both brand and generic drugs, the achievement of consistent quality and therapeutic performance using drug delivery systems can also pose serious challenges in developing a drug for the market, which requires close collaboration among industry, academia, and regulatory agencies. With the advent of personalized medicines, there will be great opportunities and challenges in utilizing drug delivery systems to provide better products and services for patients.

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