Authors:

Valeria Certuche Sanchez

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Acromegaly is a chronic endocrine disorder resulting from pituitary adenomas that trigger excessive secretion of growth hormone (GH), leading to elevated insulin-like growth factor 1 (IGF-1) levels and serious systemic complications. Octreotide, a synthetic somatostatin analog, is the first-line pharmacological treatment. Although traditionally administered via injection due to its poor intestinal permeability and enzymatic instability, recent technologies have enabled the development of oral formulations. Although peptide-based drugs like octreotide offer high potency and receptor specificity, oral administration remains a major challenge, impacting patient compliance and quality of life in long-term therapies. One promising strategy to overcome these barriers is the incorporation of permeation enhancers (PEs) into oral formulations. We have been exploring formulation strategies for the oral delivery of octreotide using intestinal permeation enhancers, specifically salcaprozate sodium (SNAC) and palmitoylcarnitine (PC), while also evaluating some surface activity parameters of these excipients in relation to their effects on permeability. The experimental groups included octreotide alone (100 µM) and combinations with SNAC (10 and 20 mM) or PC (0.1 and 0.5 mM), aiming to assess their synergistic effects on transport across the intestinal barrier. These formulations are being tested for chemical stability under acidic (pH 2.2, KH2PO4) and neutral (pH 7.4, PBS) conditions. Degradation was monitored by reverse-phase high-performance liquid chromatography (RP-HPLC) at 220 nm. Intestinal permeability has been tested using an in vitro model simulating the intestinal epithelium, based on Caco-2 monolayers cultured for 21 days on Transwell® inserts. The integrity of the monolayers was monitored by measuring transepithelial electrical resistance (TEER), † Presenting Undergrad Author; ‡ Contributing Undergrad Author; * Undergrad Acknowledgment serving as an indicator of tight junction function. Expected outcomes include the quantification of apparent permeability coefficients Papp to compare the effectiveness of each enhancer in promoting octreotide transport across the intestinal model. Keywords: Peptide Drugs; Oral Peptide Delivery; Permeation Enhancers; Caco-2 Cell; Formulation

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Purdue University / 2025

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Co-authors:

Valeria Certuche Sanchez