End-Site-Specific Conjugation of Enoxaparin and Tetradeoxycholic Acid Using Nonenzymatic Glycosylation for Oral Delivery

Administration of drugs through the oral route is considered the simplest and most convenient way to offer greater patient compliance than other routes. Most active drugs discovered in the past and those being discovered in recent times are inadequate because of their inherent limitations in physicochemical properties such as low solubility and permeability, resulting in poor bioavailability, especially after oral administration in the form of tablet or capsule. Pharmaceutical nanoemulsion is the most promising, safer, and multimodal technique for delivering poorly soluble drugs and gaining more attention due to its characteristics such as higher solubilisation capacity, smaller size, surface charge, and site-specific drug targeting. This chapter focuses on the biological fate of nanoemulsion after oral administration and a few case studies related to the oral application of nanoemulsion in delivering poorly soluble drugs. In addition, the anatomy and physiology of the GI tract, components of nanoemulsion, and methods of preparation are addressed.

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Antibody conjugation and formulation

Antibody Therapeutics ◽

10.1093/abt/tbz002 ◽

2019 ◽

Vol 2 (1) ◽

pp. 33-39 ◽

Cited By ~ 2

Author(s):

Nathan J Alves

Keyword(s):

Oral Delivery ◽

Clinical Implementation ◽

High Concentration ◽

Site Specific ◽

Routes Of Administration ◽

Drug Conjugates ◽

Large Size ◽

Low Concentrations ◽

Antibody Conjugates ◽

Antibody Conjugation

ABSTRACT In an era where ultra-high antibody concentrations, high viscosities, low volumes, auto-injectors and long storage requirements are already complex problems with the current unconjugated monoclonal antibodies on the market, the formulation demands for antibody-drug conjugates (ADCs) are significant. Antibodies have historically been administered at relatively low concentrations through intravenous (IV) infusion due to their large size and the inability to formulate for oral delivery. Due to the high demands associated with IV infusion and the development of novel antibody targets and unique antibody conjugates, more accessible routes of administration such as intramuscular and subcutaneous are being explored. This review will summarize various site-specific and non-site-specific antibody conjugation techniques in the context of ADCs and the demands of formulation for high concentration clinical implementation.

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Engineered Site-specific Vesicular Systems for Colonic Delivery: Trends and Implications

Current Pharmaceutical Design ◽

10.2174/1381612826666200813132301 ◽

2020 ◽

Vol 26 (42) ◽

pp. 5441-5455

Author(s):

Honey Goel ◽

Karan Razdan ◽

Richu Singla ◽

Sushama Talegaonkar ◽

Rajneet Kaur Khurana ◽

...

Keyword(s):

Lipid Bilayers ◽

Targeted Delivery ◽

Oral Delivery ◽

Low Cost ◽

Lipid Vesicles ◽

Oral Route ◽

Peptidase Activity ◽

Colonic Delivery ◽

Site Specific ◽

Drug Degradation

Steering drug-loaded, site-specific, coated lipid vesicles to the target receptor sites have the potential of plummeting adverse effects and improving the pharmacological response in diverse pathologies of the large bowel, especially the colon. Colonic delivery via oral route has its own challenges, often governed by several glitches such as drug degradation or absorption in the upper GIT, instability of proteins/peptides due to high molecular weight, and peptidase activity in the stomach. Consequently, colon-specific coated liposomal systems (CSLS) offer a potential alternate for not only site-specificity, but protection from proteolytic activity, and prolonged residence time for greater systemic bioavailability. On the other hand, liposomal delivery via the oral route is also cumbersome owing to several barriers such as instability in GIT, difficulty in crossing membranes, and issues related to production at the pilot scale. New advancements in the field of CSLS have successfully improved the stability and permeability of liposomes for oral delivery via modulating the compositions of lipid bilayers, adding polymers or ligands. Despite this ostensible propitiousness, no commercial oral CSLS has advanced from bench to bedside for targeted delivery to the colon as yet. Nevertheless, CSLS has quite fascinated the manufacturers owing to its potential industrial viability, simplistic and low-cost design. Hence, this review aims to decipher the convolutions involved in the engineering process of industrially viable CSLS for colonic delivery.

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