Research ArticlesEpithelial Transport and Bioavailability of Intranasally Administered Human Growth Hormone Formulated with the Absorption Enhancers Didecanoy‐L‐α‐phosphatidylcholine and α‐Cyclodextrin in Rabbits
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Human growth hormone: New delivery systems, alternative routes of administration, and their pharmacological relevance
2011, European Journal of Pharmaceutics and BiopharmaceuticsCitation Excerpt :In summary, surfactant materials and bile salts have been shown to enhance GH bioavailability. However, the enhancing effect is usually correlated to the damage caused to the nasal membrane; although for other enhancers such as cyclodextrins, chitosan and selected phospholipids (e.g., LCP), the absorption enhancing effect is reported to outweigh irritation to the mucosa [49,50,52]. The possibility of delivering therapeutic amounts of GH by the intranasal route will depend on the quantities that can be dosed in a patient-friendly system and the potential nasal and systemic toxicity of the selected enhancer material.
Reestablishment of the nasal permeability barrier to several peptides following exposure to the absorption enhancer tetradecyl-β-D-maltoside
2010, Journal of Pharmaceutical SciencesCitation Excerpt :Therefore, agents known as absorption or permeation enhancers have been added to nasal formulations containing peptides to facilitate their absorption into the systemic circulation.5–7 Successful peptide drug absorption from the nasal route has been achieved with several reagents, including chitosan, didecanoyl-L-alpha-phosphatidylcholine, dimethyl-β-cyclodextrin, and the alkylglycosides.8–11 The alkylglycosides are a family of nonionic surfactants, consisting of alkyl chains of various lengths (6–16 carbon units in length) linked to a monosaccharide (6–12 carbon unit chains) or disaccharide (10–16 carbon unit chains) moiety.12
Nasal absorption of metoclopramide from different Carbopol<sup>®</sup> 981 based formulations: In vitro, ex vivo and in vivo evaluation
2006, European Journal of Pharmaceutics and BiopharmaceuticsIntranasal delivery of recombinant human growth hormone (somatropin) in sheep using chitosan-based powder formulations
2005, European Journal of Pharmaceutical SciencesCorrelation of tetradecylmaltoside induced increases in nasal peptide drug delivery with morphological changes in nasal epithelial cells
2004, Journal of Pharmaceutical SciencesCitation Excerpt :After cooling, blocks were cut into regular or thin sections and post-stained with toludine blue for LM or uranyl acetate and lead citrate for electron microscopy and viewed on a light microscope (Nikon labophot-2, Melville, NY) or two transmission electron microscopes (model 1200 EX II and JEM-100 CX TEMSCAN microscope, Tokyo, Japan). Samples were evaluated by three investigators for signs of morphologic alterations as described previously (i.e., cellular rearrangement or denudement, pyknotic nuclei, and cilia alterations).17 These evaluations were done in order to assess the level of acute toxicity which might be expected in tissue exposed to TDM.
Thiomers in noninvasive polypeptide delivery: In vitro and in vivo characterization of a polycarbophil-cysteine/glutathione gel formulation for human growth hormone
2004, Journal of Pharmaceutical SciencesCitation Excerpt :Because nasal permeability decreases rapidly for hydrophilic molecules >1 kDa, the absorption of polypeptides such as hGH with a molecular mass of 22 kDa is negligible. To improve the nasal absorption of large‐size molecules, permeation enhancers must be included in drug formulations.23 In first orientating permeation studies, the potential of the PCP‐Cys/GSH system as an alternative nasal permeation enhancer was evaluated using FD‐4, because it is a well‐characterized paracellular marker and exhibits the advantageous property of not being enzymatically degraded in comparison to polypeptides.