Mucosal Drug Delivery Technology

With the development of medical and health industry, mucosal administration has become a research hotspot because of its convenient route of administration and good patient compliance. At present, a variety of chemical small molecule drugs can be delivered through the mucosa. At BOC Sciences, we provide development services of small molecule drugs for mucosal delivery, as well as mucosal delivery proteins and mucosal delivery hormones. Our company is focused on developing and optimizing mucosal drug delivery technologies to improve drug bioavailability and open up new pathways for drug discovery and patient treatment.

What is mucosal drug delivery system?

Mucosal drug delivery system (MDDS) is a new type of drug delivery system, which mainly refers to the drug administration mode in which drugs and appropriate carrier materials are applied to the mucosal part of the cavity to play a local effect or absorb into the systemic circulation to induce systemic therapeutic effect. The mucosal drug delivery system includes multiple pathways, such as oral mucosa, nasal mucosa, ocular mucosa, lung (inhalation), rectal mucosa, and vaginal mucosa. The mucosal system is an important protective barrier on the human surface, and it is also an important way for foreign microorganisms to infect and drug molecules to enter the human body. Compared with the ordinary skin environment, the mucosal layer does not have a keratinized surface, but only contains a single or several layers of epithelial cells, which is conducive to the transmembrane transport of drug molecules.

Mucoadhesive buccal tablets. (Mishra, R., 2021)

Advantage of mucosal drug delivery system

Compared with oral administration, drugs are absorbed into the systemic circulation through the mucosa without passing through the liver, which can effectively avoid the first passage of the liver.

The types and quantities of enzymes in the mucosa are limited, and the enzymatic degradation of drugs is relatively low.

Local administration can increase drug concentration at the site of action and improve bioavailability.

Local application, convenient for patients to operate autonomously, improve patient compliance.

Our mucosal drug delivery system development service

Types of mucosal preparations we can offer

We offer traditional mucosal dosage forms for development, including:

Gel: After the drug is mixed with specific excipients to make a gel, it can increase the adhesion of the drug on the mucosal surface and promote its entry into the body to play a curative effect. For example, after adding pectin to fentanyl, a special nasal spray device will automatically form a gel in the nasal cavity and quickly absorb into the blood.

Spray: After the drug is made into a spray, it can be attached to the mucosal surface of various cavities. For example, azolastine hydrochloride can be used as a nasal spray to significantly reduce choline-induced tracheal smooth muscle contraction in isolated bronchial smooth muscle studies in rats.

Aerosol: Aerosol can be used in respiratory tract, skin or other lumen for local or systemic treatment, and has become an indispensable dosage form in pharmaceutical preparations. The aerosol containing insulin was put into a special drug delivery device and attached to the buccal mucosal surface in the form of droplets, which could be used as a new drug delivery method instead of insulin injection.

Microsphere: The microsphere has strong adhesion and prolongs the contact time between drug and mucosa. Features that protect the drug from enzyme metabolism, thereby improving the bioavailability of mucosal drug delivery. Using hydroxypropyl methylcellulose as bioadhesive, tramadol hydrochloride was made into microspheres for nasal administration, which could efficiently transfer drugs into the brain without damaging the nasal mucosa.

Liposome: Encapsulation of drugs into liposomes can not only effectively reduce the irritation and toxicity of drugs to the mucosa, avoid the degradation of drugs by enzymes, but also make it easier for drugs to play a therapeutic effect through the phospholipid bilayer. The use of chitosan as a liposomal modification material can increase the contact time between drugs and cornea without causing mucosal toxicity to the cornea, and chitosan can be used as a carrier material for mucosal drug delivery.

Nano formulation: The particle size of nano preparation is smaller than that of microspheres, it is easier to penetrate mucosal cells, and the organism has a good tolerance to nano preparation, so this dosage form is of great value for mucosal administration. We can prepare nanoparticles with chitosan as the carrier, which can exert the effect of drugs through the cornea through cellular bypass mechanism and transcellular mechanism.

Emulsion: The droplet dispersion of the emulsion is large, and it is easier for the drug to penetrate the mucosa after the drug is made into the emulsion. We can make various drugs into emulsions for nasal mucosa, oral mucosa or eye administration. We also offer nano emulsion development.

Oral dissolving film: According to dissolution time and dissolution situation, oral soluble film can be divided into quick-release type, slow-release type of mucosal adhesion and dissolving type of mucosal adhesion. The quick-release type is usually a single film and acts on the tongue, while the slow-release type of mucosal adhesion and dissolving type of mucosal adhesion act on the gum or buccal mucosa. We use solvent casting, extrusion, freeze-drying technology and 3D printing technology to prepare oral soluble films, and test drug properties, mechanical properties, content uniformity, dissolution, microbial limits, etc.

Increasing mucosal absorption methods at BOC Sciences

Mucosal adhesion strategy: It means that drugs are loaded with adhesive polymers as carriers, adhere to the mucus for a long time through the biological adhesion of the carriers, and enter the site of action or the circulatory system through contact with the mucosal epithelium to exert local or systemic therapeutic effects. The molecular chain of the adhesive material penetrates with the viscous chain segment in the mucus. Through the comprehensive action of mechanical mosaics, van der Waals force, electrostatic attraction, covalent bond, hydrophobic action and hydrogen bond, the polymer material is provided with the opportunity to contact the mucosa, thus bioadhesion occurs and maintains for a certain time, so that the drug penetrates into the tissue and reaches the action site.

Absorption enhancers: Chemical absorption enhancers promote drug penetration through the mechanism of improving drug permeability coefficient, extracting intercellular lipids, and prolonging drug retention time on mucosal surface. Including a variety of polymer materials, cholate, sodium caprylate, caprylate and its derivatives.

Enzyme inhibitors: The mucosal surface is often distributed with a variety of enzymes, these enzymes have a certain degradation effect on the drug attached to the mucosal surface, which will lead to the drug can not play a role. Therefore, the addition of various enzyme inhibitors to mucosal medication can alleviate the degradation of drug efficacy and indirectly increase the effect of drug efficacy.

Why choose BOC Sciences?

• For the development of oral mucosal drug delivery agents, we use a unique bioadhesion system, which can be continuously and firmly attached to the oral mucosa to ensure the effective release of drugs. In addition, using transdermal accelerators and enzyme inhibitors, the company has developed a series of rapidly dissolving thin film formulations that rapidly release active ingredients and avoid first-pass effects, improving drug utilization.
• For the nasal mucosa, we have developed a highly permeable formula and microfluidic technology, which is especially suitable for the treatment of central nervous system diseases. The drugs can quickly cross the blood-brain barrier and reach the central target, providing a new treatment path for schizophrenia, Alzheimer's disease and other diseases.
• Our mucosal drug delivery technology covers a wide range of drug forms, including nanoparticles, microspheres, gels and films.
• Deep expertise and practical experience in the field of liposome development.
• Advanced equipment and facilities: Pharmaceutics laboratory, clinical pharmacokinetics laboratory and bioanalytical laboratory.

FAQ

1. What is the application and mechanism of chitosan in mucosal drug delivery?

Chitosan has good biocompatibility, biodegradability and non-toxicity, which makes it an ideal drug carrier material. The cationic properties of chitosan enable it to have strong electrostatic interactions with mucus, anionic surfaces, and other macromolecules (such as DNA), thereby enhancing the penetration of the drug in the mucosa.

2. How to solve the problem of drug penetration in mucosal drug delivery?

Use penetration enhancers. Developing novel formulation technologies, such as nanoparticles, liposomes, etc. The molecular structure of the drug is modified to improve its permeability.