1. Excellent in Quality, Competitiveness and Care
Biopharmaceutics

2.  Mucosal lining:
› Mucous ? Mucin ?
› Functions
 Epithelia 
› Thickness
› “wear and tear”stratified epithellia
› Keratinised-non keratinised epitelium

3.  Drug potency  consider the site of
administration
 Delivery form  release pattern
 Drug solubility  aqueous solubility – lipid
solubility  balance of hydrophilicity and
lipophilicity  partition and difusion
 Mucus- drug interaction
 Drug stability  consider the enzymatic
metabolism
 Degree of ionization  pKa  unionized
form absorbed

4.  Permeability
 Blood supply 
› High vasculature
› Blood flow

5. Oral administration vs oral cavity administration

6. Taken from Florence AT, Attwood D“Physicochemical Principles of Pharmacy”
- only for study purpose

7.  Buccal delivery
 Sublingual delivery
 Oropharyngeal delivery
 Periodontal delivery

8.  Avoidance of GIT hazardous
environment
 Avoidance of First Pass Hepatic
Elimination  there are no hepatic
portal veins  direct access to the
systemic circulation via internal jugular
vein
 Adequate vasculature and blood supply
 Relatively permeable
 Rapid onset  sublingual delivery
 Sustained release  buccal delivery

9.  Epithelial cell layer and mucous layer
thickness
 Mucous and saliva mobility

10.  Saliva movement and dilution
 Enzymatic barrier
 Thickness of mucosal layer
 Limited surface area
 Lipoidal barrier of buccal

11.  Mucoadhesive polymer
 Enzyme inhibitor
 Penetration enhancer
 Chemical modification

12.  Chewing formulation
 Fast release dosage form
 Mucoadhesive dosage form

14.  Eyelid
› Keep the tear film and lacrimal drainage
 Cornea
› Site of drug administration transcorneal absorption
› Epithelium-stroma-endothelium
 Conjunctiva
› Conjunctiva sac (the inferior one  “cul de sac”)(also) site of
drug instillation
› Drug absorption site
 Aqueous humor
 Iris-lens
› Light entry regulation
 Vitreous body and vitreous humor
› Keep the retina pressed against choroid
 Retina
› Visual acuity, nerves
› Configuration of photoreceptor cells
› Blood retinal barrier efflux system and tight junction on:
 Endothelium on retinal vessel
 Retinal Pigmented Epithellium (RPE) cells

15.  Ways to across the blood eye barrier
and cornea
› Blood-eye barrier
› Cornea
 Localisation the action at the eye
 Retention time while reducing the
frequency of instillation

16.  Safe and effective
 Sterile
 Certain criteria for certain dosage form:
› Pyrogen-free  parenteral administration
› Isotonic-Isohydris,
› free from particles solution (eyedrop-
injection)
› Free from large particles suspension-
ointment
› Free from foreign matters
 Advanced carrier  biodegradable

17.  Corneal penetration
 Noncorneal, productive ocular
absorption  conjuntival-scleral
absorption hydrophilic compounds
› Conjunctiva and sclera are more
permeable than cornea
› Could be non-productive if penetration
through conjunctival blood vessels occurs
 Noncorneal, non productive absorption,
› Conjuctival vessels  systemic
› Precorneal drainage (role of
hydrodynamic)80-90% drug removed

18.  Force out the matters from the eye and
perform nasolacrimal drainage
 Explain the effect of excessive
instillation:
› Bitter taste after instillation
› Systemic effect via GI absorption
 Suggest :
› the volume of eye drop administration (5-
10L/drop)
› The use of mucoadhesive carrierprolong
the residence time

19.  Solubility and partition coefficient
 Molecular weight
 State of ionisation and pH
 Protein binding
 Pigmentation and drug effect

20.  Proper placement of the dosage form
 Instillation volume
 The use of mucoadhesive polymer and
in situ gelling forming  viscosity
enhancement

21.  Mydriatics and Cycloplegics
 Miotics
 Anti-inflammation
 Anti bacterial-antifungal
 Anti-glaucoma
 Age related macular degeneration
 Dry eyes  artificial tears

22.  Most commonly used  benzalkonium
chloride (in a concentration of 0,01%);
 Role: microbial growth controller, it can
also be used as penetration enhancer
 Limitation:
› If the concentration exceeded, may cause
irritation/corneal damage).
› incompatible for salt form active
ingredientanionic-cationic interaction)
 Other organic mercurials careful
with the side effect of mercury!

23.  Intravitreal administration
 Subconjunctival administration
 Periocular administration
› Sub Tenon’s capsule administration
› Retrobulbar injection

25.  Local therapy, example…
 Systemic therapy, especially in condition:
› Unable for oral administration
› Unconscious
› Unacceptable taste
› Unstable against GI hazardous environment
 Advantages :
› Non invasive; can be self administered
› For systemic :
 High vasculature
 Permeability
anatomy

26.  Suppositoria
 Rectal gel:
 Enema

27. Microlax ?
www.drugs.com

28.  Bases:
› Fatty base (melted) cocoa butter; adeps
solidus; witepsol
› Water soluble base (dissolved)  osmotic
effect hygroscopic
› Glycero-gelatine base  hygroscopic
 Consideration:
› Melting point
› Solidification rate
› API-excipient affinity/interaction

29.  Local therapy, mostly related to
antibiotics-antifungi
 Points for systemic delivery:
› Blood supply
› Permeability
› Hepatic FPE avoidance
› Less protease

30.  Ethic issues
 Erratic absorption due to epithellium
thickness variation as the consequences
of menstrual cycles
 Mucus as physical barriers