MUCOADHESIVE BIOTECHNOLOGY:

PERSPECTIVES

Ch. Tzachev & T. Popov, 2004

Principle of mucoadhesiveness:

To prolong the contact time between

drugs and the mucosa so as to increase

their bio-availability, and, subsequently,

their efficacy.
Mucoadhesive carriers:

• Solutions
• Powders

• Gels

• Microspheres

• Liposomes
Advantages of
mucoadhesive solutions:

• Low viscosity and significant

adhesiveness.
• Good tolerability.
• Reduced active drug dosage and/or
decreased number of applications.
• Lower cost.
Rationale: Standard case
of drug application
on mucosa

Drug

mucosa

blood
Rationale: Mucoadhesive
technology

Mucoadhesive solution + drug

Interpenetration

Prolonged contact with the mucosa

↑ Bioavailability
blood
Applications of mucoadhesive solutions:

nose

• Decongestant
(Xylometazoline)
– Allergic rhinitis
Tzachev et al, Br J Clin Pharm, 2002

– Viral infections

1
Applications of mucoadhesive solutions:

nose

• Antiemetics
(Clopramide, 5-HT4 agonist )

Tzachev CT. PhD thesis. 2003.

2
Applications of mucoadhesive solutions:

nose

• Second generation H1 antagonist

(Loratadine)

Unpublished results

3
Applications of mucoadhesive solutions:

nose

• Nasal corticosteroids

– Allergic rhinitis
– Nasal polyposis

4
Applications of mucoadhesive solutions:

nose

• CNS drugs
– pain-killers
– sleep promoting drugs
– cerebral vasodilators
– cerebral stimulants

5
Applications of mucoadhesive solutions:

• Antiseptics

• Local steroids Pharynx & larynx

• Anesthetics

• Cytostatics

6
Applications of mucoadhesive solutions:

• Lower airways

– Asthma
– COPD Lower
airways

7
Applications of mucoadhesive solutions:

Other:
• Sublingual
• Gastro-intestinal tract
• Conjunctivae
• Vaginal cavity
• Skin lesions
• Slow healing wounds
8
Technical aspects:

• For each different formula the specific

conditions need to be adjusted in order to
obtain optimal results.

• Methodology and original devices to

measure viscosity and mucoadhesiveness
needed.
Administrative and economic aspects:

• The mucoadhesive technology has been

developed for existing drugs.

 Approval
 Licensing
 Investment
Administrative and economic aspects:

• The mucoadhesive technology has been

Theexisting
developed for combination
drugs.
drug + mucoadhesive
may possess new qualities,
which may exceed
the benefits
 Approval
from
 the drug itself
Licensing
 Investment
1
Economic aspects:

• Low cost of the ingredients