ATUL CHAUDHARY STUDENT (M.PHARM, PHARMACEUTICS) ISF, COLLEGE OF PHARMACY, GHALKALAN MOGA, PUNJAB (BEST SLIDE FOR PREPRATION OF PHOSPHOLIPID TOPIC SPECIALLY FOR MASTER STUDENTS, AS WELL AS GRADUATION STUDENTS)

1. Seminar Presentation
ISF COLLEGE OF PHARMACY MOGA
Presented By;
Atul Chaudhary
M.Pharm. 1st year
Pharmaceutics

2. PHOSPHOLIPIDS
 Phospholipids are a class of lipids that are a
major components of all cell membrane.
 They can form lipid bilayers because of their
amphiphilic characteristics.
 The structure of the phospholipids molecules
generally consists of two hydrophobic fatty acids
‘tails’ and a hydrophilic ‘head’ consisting of a
phosphate group.
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3. SYNTHESIS OF PHOSPHOLIPIDS
 Phospholiopids are synthesized from
phosphatidic acid and 1,2-diacylglycerol,
intermediates in the production of
triacylglycerols.
 Phospholipds synthesis occurs in the smooth
endoplasmic reticulum.
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4. FUNCTIONS OF PHOSPHOLIPID
 In association with proteins phospholipids
from the structural components of membranes
and regulate membrane permeability.
 They participate in the absorption of fats from
the intestine.
 They are essential for the synthesis of
different lipoproteins and thus particulate in
transport of lipids.7 February 2020 PHOSPHOLIPID COMPLEX 4

5. PHOSPHOLIPID BILAYER
 In water, the interactions of the hydrophobic
tails and hydrophilic heads of phospholipids
generate a phospholipids bilayer that is two
molecules thick.
 The head groups are directed outwards, where
they interact with the surrounding water.
 The tails are packed together in the interior of
the bilayer.7 February 2020 PHOSPHOLIPID COMPLEX 5

6. 7 February 2020 PHOSPHOLIPID COMPLEX 6
PHOSPHOLIPID BILAYERS

7. AMPHIPHILIC CHARACTER
 An amphiphile is a term describing a chemical
compound possessing both hydrophilic (water-loving,
polar) and lipophilic (fat-loving, non-polar) properties.
 The phospholipids head are hydrophilic and interact
towards the water The phospholipids tails are
hydrophobic and avoid interactions with water.
 These specific properties allow phospholipids to play
an important role in the phospholipids Bilayer.
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8. 7 February 2020 PHOSPHOLIPID COMPLEX 8
SPHINGOLIPIDS Contd…

9. cleavage at the SN-1 or SN2 position of
phospholipids.
2. Phospholipase A2 is positions of glycerol
backbones.
3. Phospholipase C are founds in enzyme linked
receptors and IP 3 pathway
4. phospholipse D have been identified in
mammalian cells.
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10. WHAT IS PHOSPHOLIPID COMPLEX
 Low bioavailability of drugs is due to presence of P-gap
pump which causes the efflux of naked drugs, the
presence of metabolizing enzymes, and the environmental
pH-mediated degradation.
 Thus, delivery vehicles are essential for drugs so as to
attain a desired level in the systemic circulation .
Phospholipid-drug complex could be used for the same, in
which the absorption process is similar to the process
through which the triglycerides and essential
phospholipids are absorbed.
 The mechanism for absorption of the phospholipid-drug7 February 2020 PHOSPHOLIPID COMPLEX 10

11. STRUCTURE OF PHOSPHOLIPID COMPLEX
 Structurally, the phospholipid comprises two fatty acid
chain attached to the glycerol (dactyl glycerol) moiety,
which undergoes hydrolysis to release fatty acid, which
triggers its absorption.
 Similarly, the drug-dactyl glycerol complex when taken via
oral route undergoes hydrolysis. Minor hydrolysis occurs
in the stomach at pH of ~ 1.5, and majority of it occurs in
the intestine starting from duodenum in which secretions
from the liver, bile bladder, and pancreas in the form of
juice are secreted.7 February 2020 PHOSPHOLIPID COMPLEX 11

12. HOW BIOAVAILABILITY ENHANCEment ?
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13. METHODS OF PREPRATION OF PHOSPHOLIPID COMPLEX
 Solvent evaporation
 Super critical fluid (SCF) process
 Co-solvent lyophilization
 Anti-solvent precipitation
 Co-grinding
CURRENT TRENDS IN PHOSPHOLIPID-DRUG COMPLEXES:-
 Solubility Enhancement
 Increased GIT Metabolic Stability
 Permeability Enhancement
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14. 1. SOLVENT EVAPORATION METHODS :-
Drug and phospholipid are mixed in
solvent/mixture of solvent in different ratio
followed by solvent evaporation by rota
evaporation.
2. SUPER CRITICAL FLUID PROCESS :-
USING SUPERCRITICAL FLUIDS Like carbon dioxide
3. ANTI-SOLVENT PRECIPITATION :-
Solvent evaporation by freeze drying use of anti
solvent to precipitate drug phospholipid
complex.
4. MECHANICAL DISPERSION/SONICATION CO-GRINDING :-
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Contd…

15. BIOPHARMACEUTICAL CLASSIFICATION SYSTEMS (BCS)
CLASS I CLASS II
CLASS III CLASS IV
BCS
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PERMEABILITY
SOLUBILITY
HS, HP LS, HP
HS, LP
HS = High solubilitty
HP = High permeability
LS = Low solubility
LP = Low permeability
LS, LP

16. SOLUBILITY BASED CLASSIFICATION OF DRUGS
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17. EVALUATION OF Phospholipid COMPLEX
1. SPECTROSCOPY :- Complex formation and interactions is
associated with some characteristic signals studied by
employing different spectroscopic techniques like 1H-
NMR, 13C-NMR, and IR spectroscopy.
2. DRUG contents:- Weighed quantity equivalent to 10 mg
complex was added to 50 ml phosphate buffer in beaker.
The contents were stirred on a magnetic stirrer for 4
hours and then allowed to stand for one hour. Clear liquid
was decanted and centrifuged at 5000 rpm for 15
minutes. supernatant was filtered suitable dilution
absorbance was measured in UV at 257 nm .
3. Particle size distribution :- Average particle size varied between
684 nm to 1628 nm . The results indicate that as the7 February 2020 PHOSPHOLIPID COMPLEX 17

18. 3. SOLUBILITY :-
The solubility of a solid substance is defined as
the concentration at which the solution phase is
in equilibrium with a given solid phase at a
stated temperature and pressure. The solubility
of a candidate drug may be the critical factor
determining its usefulness.
4. PHARMACOKINETIC STUDIES :-
The main pharmacokinetic parameters
Maximum concentration (Cmax) and time to
reach maximum concentration (Tmax) are the
values obtained directly from concentration–
time curve. Area under the concentration–time
curve (AUC0–tn and AUC0–t), elimination half7 February 2020 PHOSPHOLIPID COMPLEX 18
Contd…

19. SOME OTHER techniques
 Fourier transform infrared spectroscopy (FTIR)
 Differential scanning calorimetry (DSC)
 X-Ray diffraction (XRD) study
 Scanning Electron Microscopy (SEM)
 Transmission electron microscopy (TEM)
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20. CONCLUSIONS
 In the present study, an attempt was made to
enhance the aqueous solubility of drugs via its
complexation with phospholipids.
 The prepared complex were evaluated for
physicochemical, functional, and pharmacological
attributes.
 The FTIR, DSC, PXRD, photomicroscopy, and the
SEM studies indicated the successful formation of
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21. REFERENCEs
 Jain S, Jain V, Mahajan SC. Lipid based vesicular
drug delivery systems. Adv Pharm. 2014;2014:1–
14. doi: 10.1155/2014/574673
 Devi VK, Jain N, Valli KS. Importance of novel
drug delivery systems in herbal
medicines. Pharmacogn Rev. 2010;4(7):27–31. doi:
10.4103/0973-7847.65322.
 Lipid based drug delivery strategies for oral drug
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