Biopharmaceutics

Biopharmaceutics, in connection with pharmacokinetics, is the field that investigates and describes everything that happens with a medicinal product and the active substance between the moment of administration, the moment it exerts its action and the moment it is eliminated from the body. Biopharmaceutics connects the physico-chemical properties of an active substance and its dosage form, especially through the drug release characteristics, with its fate and action in the living organism. Actually biopharmaceutics describes how medicine formulation technologies can affect pharmacokinetics and pharmacodynamics. The route of administration, the way the active substance is released from the dosage form, and the way the body handles (absorbs, distributes, metabolises and excretes) the active substance, together determine its (duration of) action, its efficacy and the occurrence of adverse effects. This chapter explains general principles of biopharmaceutics and its relation to pharmacokinetics in the light of their implications on the design of medicines. It describes the general biopharmaceutical principles that are relevant to the major routes of administration: parenteral, oromucosal, oral, rectal, dermal, nasal, pulmonary and ocular. Topics discussed include solubility and dissolution, bioavailability, partition coefficient and pH partition theory, the biopharmaceutical classification system (BCS), excipient-, food-, drug- and herb-drug interactions, first-pass effects and drug metabolism, bioequivalence and new developments in the field of advanced drug delivery systems.</p

Biopharmaceutics

Biopharmaceutics, in connection with pharmacokinetics, is the field that investigates and describes everything that happens with a medicinal product and the active substance between the moment of administration, the moment it exerts its action and the moment it is eliminated from the body. Biopharmaceutics connects the physico-chemical properties of an active substance and its dosage form, especially through the drug release characteristics, with its fate and action in the living organism. Actually biopharmaceutics describes how medicine formulation technologies can affect pharmacokinetics and pharmacodynamics. The route of administration, the way the active substance is released from the dosage form, and the way the body handles (absorbs, distributes, metabolises and excretes) the active substance, together determine its (duration of) action, its efficacy and the occurrence of adverse effects. This chapter explains general principles of biopharmaceutics and its relation to pharmacokinetics in the light of their implications on the design of medicines. It describes the general biopharmaceutical principles that are relevant to the major routes of administration: parenteral, oromucosal, oral, rectal, dermal, nasal, pulmonary and ocular. Topics discussed include solubility and dissolution, bioavailability, partition coefficient and pH partition theory, the biopharmaceutical classification system (BCS), excipient-, food-, drug- and herb-drug interactions, first-pass effects and drug metabolism, bioequivalence and new developments in the field of advanced drug delivery systems.</p

Biopharmaceutics

Biopharmaceutics, in connection with pharmacokinetics, is the field that investigates and describes everything that happens with a medicinal product and the active substance between the moment of administration, the moment it exerts its action and the moment it is eliminated from the body. Biopharmaceutics connects the physico-chemical properties of an active substance and its dosage form, especially through the drug release characteristics, with its fate and action in the living organism. Actually biopharmaceutics describes how medicine formulation technologies can affect pharmacokinetics and pharmacodynamics. The route of administration, the way the active substance is released from the dosage form, and the way the body handles (absorbs, distributes, metabolises and excretes) the active substance, together determine its (duration of) action, its efficacy and the occurrence of adverse effects. This chapter explains general principles of biopharmaceutics and its relation to pharmacokinetics in the light of their implications on the design of medicines. It describes the general biopharmaceutical principles that are relevant to the major routes of administration: parenteral, oromucosal, oral, rectal, dermal, nasal, pulmonary and ocular. Topics discussed include solubility and dissolution, bioavailability, partition coefficient and pH partition theory, the biopharmaceutical classification system (BCS), excipient-, food-, drug- and herb-drug interactions, first-pass effects and drug metabolism, bioequivalence and new developments in the field of advanced drug delivery systems.</p

Gemcitabine and glioblastoma: challenges and current perspectives.

Gemcitabine is a nucleoside analog currently used for the treatment of various solid tumors as a single agent or in combination with other chemotherapeutic drugs. Its use against highly aggressive brain tumors (glioblastoma) has been evaluated in preclinical and clinical trials leading to controversial results. Gemcitabine can inhibit DNA chain elongation, is a potent radiosensitizer and it can enhance antitumor immune activity, but it also presents some drawbacks (e.g., short half-life, side effects, chemoresistance). The aim of this review is to discuss the challenges related to the use of gemcitabine for glioblastoma and to report recent studies that suggest overcoming these obstacles opening new perspectives for its use in the field (e.g., gemcitabine derivatives and/or nanomedicines)

Specificity of pharmacokinetic modeling of nanomedicines

International audienc

Population pharmacokinetic modelling of intravenous LNCs FRET in rat

International audienc

Evaluation of lauroyl-gemcitabine-loaded hydrogel efficacy in glioblastoma rat models.

Anticancer drug-loaded hydrogels are a promising strategy for the local treatment of incurable brain tumors such as glioblastoma (GBM). Recently, we demonstrated the efficacy of lauroyl-gemcitabine lipid nanocapsule hydrogel (GemC-LNC) in a U-87 MG xenograft orthotopic mouse model. In this study, we developed a reliable and reproducible surgical procedure to resect orthotopic GBM tumors in rats. GemC-LNC hydrogel integrity was tested after brain administration in rats and its anti-tumor efficacy was tested on a 9L syngeneic orthotopic model. We demonstrated that LNC integrity is maintained at least for one week after local administration of GemC-LNC. GemC-LNC was able to delay the formation of recurrences in 9L tumor-bearing resected rats, demonstrating the efficacy of this nanomedicine hydrogel in this preclinical model. Our results confirm that GemC-LNC, a hydrogel uniquely formed by a nanocarrier and a cytotoxic drug, could be a promising and safe delivery tool for the local treatment of operable GBM tumors