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Файл:Ординатура / Хирургия / Библиотека им академика М.И. Перельмана / Книга_5320_Библиотеки_им_академика_М_И_Перельмана
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15.2 Need for Alternate, Non- oral Routes to the Systemic Circulation
Pharmaceutical Dosage Forms and Drug Delivery
upper intestine.
-
cellular passage of drug molecules from the intestinal lumen to the lamina propria.
transdermal routes of drug administration.
15.2.1 Rectal Drug Delivery
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Organ-Specic Drug Delivery
rectal administration of drugs is inconvenient and has irregular drug absorption. Moreover, rectal admin-
the formation of an abscess.
15.2.2 Vaginal Drug Delivery
intercourse.
15.2.3 Transdermal Drug Delivery
from direct penetration of the drug through the stratum corneum, deeper epidermal tissues, and the dermis.
circulation. Among the factors
enhance the
percutaneous absorption of a drug.
In general, patches are composed
types-
exemplied ®® (testosterone),
Alora® (estradiol), Androderm® ® ® is a
stratum
corneum.
15.2.4 Buccal and Sublingual Drug Delivery
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Pharmaceutical Dosage Forms and Drug Delivery
15.2.5 Nasal Drug Delivery
of nasal administration include fast absorption, rapid onset of action, and avoidance of hepatic and intes-
15.2.5.1 Barriers to Transnasal Drug Delivery
1. Physical barrier
2. Temporal barrier
3. Enzymatic barrier
calcitonin.
15.2.5.2 Drug Delivery to the Brain Through the Nasal Route
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Organ-Specic Drug Delivery
across the nasal mucosa.
15.2.5.3 Formulation Factors Affecting Transnasal Drug Delivery
1. pH-
irritation.
2. Osmolality-
dence time of the DDS at the site of absorption.
3. tion site.
4.
increase the diffusible fraction of the drug.
6.
15.3 Need for Organ- Specific and Targeted Drug Delivery
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260
15.3.1 Advantages of Targeted Drug Delivery
Pharmaceutical Dosage Forms and Drug Delivery
•
•
15.3.2 Examples of Established Drug Targeting Strategies
•
•
•
•
Targeted Delivery of Small and Macromolecular Drugs
15.3.2.1 Pulmonary Drug Delivery
through the alveoli.
15.3.2.1.1 Advantages of Pulmonary Drug Delivery
2
corticosteroids, antibiotics, antifungal agents, antiviral agents, and vasoactive drugs.
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Organ-Specic Drug Delivery
261
®
15.3.2.1.2 Barriers to Pulmonary Drug Delivery
15.4 Local Drug Delivery to the Lung
into the lung.
15.5 Systemic Drug Delivery Through the Lung
the inhaled drug in the lung.
1. Size and drug loading of the particles: Fine aerosols deposit better in the lung alveoli and periph-
particles deposit more drugs per unit surface area but tend to be deposited in the central, larger
in the alveoli.
2. Density of the particles
through the particle at the site of absorption.
3. Particle shape
can reduce the alveolar deposition of a drug.
4. Aggregation
proportion of the formulation from reaching the alveoli.
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262
Pharmaceutical Dosage Forms and Drug Delivery
Hygroscopicity
15.6 Devices for Pulmonary Drug Delivery
1. Metered dose inhaler
propellant(s), surfactant(s), and the drug in either dissolved or a suspended state in its formula-
2. Nebulizer
3. Dry powder inhaler
tracheobronchial tree.
15.6.1 Ocular Drug Delivery
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Organ-Specic Drug Delivery
263
FIGURE 15.1
spacer, illustrating the impact of a simple spacer in terms of enhanced droplet percentage reaching the tracheobronchial tree.
Q = Airow Rate
FIGURE 15.2
Targeted Delivery of Small and Macromolecular Drugs, Boca Raton,
15.6.1.1 Structure of the Eye
chamber (
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264
Pharmaceutical Dosage Forms and Drug Delivery
15.6.1.2 Routes of Drug Administration into the Eye
1. Topical route of drug administration
-
ation through the canal of Schlemm.
2. Systemic drug administration:
absorption limitation due to high intraocular pressure.
3. Intravitreal administration
vitreous humor.
4. Periocular administration
sclera and can result in high drug concentration both in the anterior and posterior segments
Retrobulbar injection
the blood vessels.
6. Peribulbar injection
tration of analgesics.
7. Subtenon injection
8. Subconjunctival injection:
segment diseases.
15.6.1.3 Challenges to Ocular Drug Delivery
(
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Organ-Specic Drug Delivery
gp), multidrug resistance- associated proteins (MRPs), and breast cancer- resistant proteins, also limits the
For drugs administered through the topical route, the cornea is the main barrier to drug absorption.
of the vitreous humor at the retinal surface.
15.6.1.4 Physicochemical Characteristics of the Drug for Ocular Absorption
1.
2.
15.6.1.5 Approaches for Enhancing Drug Delivery to the Eye
1. Prodrugs
an active drug upon absorption through various chemical bond cleavage mechanisms, such as
2. Permeability and efux pump modication
d
®®
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