Intestinal Targeted Drug Delivery System Development

At Ace Therapeutics, we specialize in the design, development, and preclinical evaluation of GI drug delivery systems. Our multidisciplinary team of formulation scientists, pharmacologists, and biomaterials experts collaborates closely with clients to overcome drug delivery challenges and accelerate drug development.

Overview of Intestinal Drug Delivery System

The gastrointestinal (GI) tract is a complex physiological environment that poses significant challenges for effective drug delivery. Factors such as pH variability, enzymatic degradation, mucus barriers, and variable transit times require sophisticated delivery strategies to ensure optimal drug absorption and therapeutic efficacy. Over the past century, advancements in pharmaceutical sciences have led to the development of innovative GI drug delivery systems that enhance bioavailability, enable site-specific release, and improve patient compliance.

Fig. 1 Schematic of preparing CUR/EMO NE by high-energy emulsification. (Lei F, et al., 2023)

What Can We Offer?

Intestinal Targeted Drug Delivery System Development Services

• Oral Controlled-Release Delivery Systems
  Our oral controlled-release technology platform encompasses three sophisticated formulation strategies to modulate drug release kinetics. Utilizing engineered hydrophilic/hydrophobic polymers, matrix-based systems create diffusion-controlled release profiles, while reservoir-type osmotic pump systems achieve consistent zero-order release kinetics for optimal therapeutic maintenance. Additionally, our delayed-release formulations incorporate pH-responsive enteric coatings that provide reliable gastric protection while enabling targeted intestinal drug delivery.
• Site-Specific Delivery Systems
  Utilizing our targeted drug delivery platform, we employ precision engineering methods to achieve site-specific release in the gastrointestinal tract. Colon-targeted systems utilize pH-sensitive polymers, time-dependent formulations, and microbiota-activated carriers featuring azo polymer scaffolds that undergo selective bacterial degradation in the colonic environment. Furthermore, our duodenal/jejunal targeting systems exploit endogenous bile acid transport mechanisms and enzyme-responsive carriers to enable efficient absorption of peptide and protein therapeutics while protecting them from proximal digestive degradation.
• Nanotechnology-Enabled Delivery Systems
  By adopting innovative formulation strategies, our nanotechnology platform overcomes key challenges in drug delivery. Liposomal and polymeric nanoparticle systems significantly enhance the solubility and intestinal permeability of poorly absorbed therapeutics, particularly effective for hydrophobic compounds like cyclosporine analogs through optimized encapsulation efficiency (>90%) and controlled release profiles. Solid lipid nanoparticles (SLNs) and nanoemulsion formulations provide exceptional physicochemical stability while promoting targeted lymphatic uptake of lipophilic actives through chylomicron-mediated transport pathways. Furthermore, our mucus-penetrating particle (MPP) technology utilizes PEGylated surface modifications and charge-shielding strategies to effectively bypass mucociliary clearance mechanisms, enabling prolonged mucosal residence and enhanced epithelial absorption.
• Stimuli-Responsive Delivery Systems Our stimulus-responsive drug delivery platform is based on an advanced activation mechanism that enables precise drug release. pH-sensitive carriers utilize tailored polymer compositions that undergo controlled dissolution at defined gastrointestinal pH thresholds (5.5-7.4), enabling segment-specific delivery to the ileum or colon with <5% premature release. Enzyme-activated systems incorporate protease- or glycosidase-cleavable linkers that respond selectively to luminal enzymatic profiles, achieving >90% payload release within targeted regions. For inflammatory bowel disease (IBD) therapeutics, our redox- and microbiota-responsive carriers exploit pathological elevations in reactive oxygen species and unique bacterial enzyme signatures to enable disease state-specific drug activation while maintaining stability in healthy tissues.
• Biologics & Peptide Delivery Systems Our innovative biopharmaceutical delivery platform combines complementary strategies to overcome gastrointestinal absorption barriers. Permeation-enhancing formulations incorporating SNAC (sodium N-[8-(2-hydroxybenzoyl) amino] caprylate) and medium-chain fatty acids significantly improve the intestinal absorption of sensitive biologics including GLP-1 analogs, insulin, and monoclonal antibodies through transient epithelial tight junction modulation. Concurrently, our enteric-protected carrier systems combine pH-responsive coatings with targeted protease inhibitors to create a protective microenvironment that shields therapeutic proteins from luminal enzymatic degradation while maintaining >90% bioactive payload integrity until reaching optimal absorption sites.

Ace Therapeutics brings together an interdisciplinary team of seasoned pharmacologists, innovative materials scientists, and formulation specialists to promote drug development from target identification to pre-clinical studies. If you are interested in our services, please do not hesitate to contact us.

Reference

1. Lei F, et al. Oral hydrogel nanoemulsion co-delivery system treats inflammatory bowel disease via anti-inflammatory and promoting intestinal mucosa repair. J Nanobiotechnology. 2023, 21(1):275.

Our products and services are for research use only and can not be used for diagnostic or other purposes.