Enzyme activated drug delivery system

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2.  INTRODUCTION
 DEFINITION
 CLASSIFICATION
 DELIVERY CARRIERS
 STRATEGIES
 APPLICATION
 REFERENCES
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3.  Type of biochemical system depends on the
Enzymatic process to activate the release of drug.
 Drug reservoir is either physically entrapped in
microspheres or chemically bound to polymer
chains from biopolymers(albumins or
polypeptides).
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 The release of drug is activated by enzymatic
hydrolysis of biopolymers by specific enzyme in
target tissue.
Ex. Albumin microspheres release 5-fluorouracil in a
controlled manner by protease-activated
bidegradation.

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An enzyme activated system, the discharge of drugs
from the system is activated by the enzymatic process.
Various approaches for enzymatic drug delivery
include liposomes, nanoparticles, prodrug,
microparticles, etc. The main components in this
system are drug, nanocarrier, promoiety, coating
polymer, ligand, etc.

6. Enzyme Activated Drug Delivery System
Activation-Modulated DDS
(2ND Generation controlled DDS)
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7.  These are the substances used to deliver the drug,
in which the drug molecule gets entrapped/linked
to its polymer chains.
 Nanotubes of carbon molecules are the effectual
carriers of the drug because they get easily
internalized by mammalian cells and acts as the
room for drugs until they reach the target cell.
 They are less preferable because of
toxic effects.
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8.  POLYMER TYPE NANOPARTICLES
 LIPOSOMES
 MESOPOROUS SILICA NANOPARTICLES
 MICROSPHERES
 PRODRUG
 CO-DRUG
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Controlled drug delivery system(microspheres)
releases the drug in controlled rate and overcome
the problems of conventional drug delivery system
and enhances the therapeutic efficacy of a drug.
The release of drug controlled by dissolution or
degradation of matrix.

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One approach towards improving the specificity of
chemotherapy is enzyme-activated prodrug therapy
in which a non-toxic drug is converted into a
cytotoxic agents, i.e. antimetabolites and alkylating
agents.
E.g. ADEPT, GDEPT

16.  Tumor Targeting
Ex.DOXORUBICIN
Doxorubicin is a type of chemotherapy drug
called an anthracycline. It slows or stops the growth of
cancer cells by blocking an enzyme called topo-
isomerase. Cancer cells need this enzyme to divide
and grow.
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17.  Conjugating the active moiety with those drugs that
will inhibit the functioning of certain efflux
transporters will improve the drug absorption into
the target site or cell with overexpressed enzyme
functioning.
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One of such examples is conjugating the anti-
neoplastic drug-like Doxorubicin with the drugs
quinidine, verapamil that inhibit the efflux
transporters like p-gp will promote the cellular
uptake of doxorubicin by temporary inactivation
of efflux transporter.
Example is conjugating the anti-neoplastic drug-
like Doxorubicin.

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 This type of drug delivery is utilized for the
treatment of various ailments including cancer.
Ex. The enzyme-activated intracellular delivery of
brilliant green using dextrin-coated halloysite
nanotubes is a promising platform for anticancer
treatment.

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The drug is supplied to the particular site,
showing action on that site thus avoiding the
unsolicited side effects on other types of tissues
or organs.
The enzyme activated drug delivery offers the
targeted release in the controlled manner.

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 A Chapter in a Book
1) Jain NK. Introduction to novel drug delivery systems.
Edn 2, Vallabh Prakashan, Delhi, 2017, pp.185
2) Baviskar DT, Jain DK. Novel Drug Delivery
Systems. Edn 4, Nirali Prakashan, Pune, 2018, pp. 2.26

22.  Journal Articles
1) Ahad HA, Haranath C, Vikas SS, Varam NJ,
KsheerasagareT, Gorantla SP. A Review on Enzyme
Activated Drug Delivery System. Research Journal of
Pharmacy and Technology. 2021 Jan 29;14(1):516-22.
2) Dzamukova MR, Naumenko EA, Lvov YM, Fakhrullin
RF. Enzyme-activated intracellular drug delivery with
tubule clay nanoformulation. Scientific reports. 2015
May 15;5(1):1-1.
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