Polymeric Nanoparticle Technologies for Oral Drug Delivery

Abstract

Biologics are being increasingly used for the treatment of many diseases. These treatments typically require repeated doses administered by injection. Alternate routes of administration, particularly oral, are considered favorable because of improved convenience and compliance by patients, but physiological barriers such as extreme pH, enzyme degradation, and poor intestinal epithelium permeability limit absorption. Encapsulating biologics in drug delivery systems such as polymeric nanoparticles (NPs) prevents inactivation and degradation caused by low pH and enzymes of the gastrointestinal (GI) tract. However, transport across the intestinal epithelium remains the most critical barrier to overcome for efficient oral delivery. This review focuses on recent advances in polymeric NPs being developed to overcome transport barriers and their potential for translation into clinical use.

Poly(amido amine) dendrimers in oral delivery

“…Particularly, the use of particulate carrier systems involving the use of lipoic and polymeric carriers has been highly successful in the field of oral delivery. 12,13 Polymeric Oral Drug Delivery Systems Drug delivery involving either chemical conjugation or physical complexation to polymeric carriers can result in prolonged circulation half-life, increased concentration at the site of action and reduced non-specific toxicity. 14,15 For oral drug delivery, polymers provide the potential advantage of protecting drugs and macromolecules against degradation in the gastrointestinal tract and enhanced uptake.…”

Nanoparticles: A Promising Drug Delivery Approach

“…However still, it is linked with a number of barriers, such as acidic pH of the stomach and digestive enzymes [58]. The nanoparticle delivery in this system occurs by transcytosis and intracellular uptake, and transport occurs through the epithelial cells lining intestinal mucosa and Peyer's patches [59].…”

Nanocarriers as treatment modalities for hypertension

“…Transcytosis being active transport pathway restricts large sized and charged molecules. When the mucosal barrier is permeated, molecules have to cross lamina propria where blood capillaries lie and molecule can get entry into the blood stream (Turner, 2009;Pridgen et al, 2014). Strategy to overcome intestinal barrier was to prepare mucoadhesive formulation which increases the contact time of the formulation with mucus thereby increasing drug concentration at the site of absorption.…”

“…M cells have less quantity of protease enzyme and lacks mucus secretion. Lipophilic molecules have improved M cell transport (Pridgen et al, 2014).…”

“…Incorporation of the drug into nanoparticles can overcome these barriers (Pridgen et al, 2014). Proteins and peptides therapeutics including insulin glargine, etanercept, cyclosporine, desmopressin, and jellyfish collagen protein (possess antihypertensive activity) are poorly bioavailable due to their charged nature, high molecular weight, low lipophilicity, and degradation by protease and peptidase secreted in the GIT.…”