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N O V EL D RU G D ELIV ERY SYSTEM

ARTICLE TYPES

NOVEL DRUG DELIVERY SYSTEM

New Novel

As a Novel

Up System

Drug Fact

About Authors:
Aruna Rastogi
Roorkee College of Pharmacy and UTU
Patanjali Ayurved Ltd, Sr. Chemist
arunarastogi10@gmail.com
1. INTRODUCTION
1.1 NOVEL DRUG DELIVERY SYSTEM:
The method by which a drug is delivered can have a significant effect on its efficacy. Some drugs have an
optimum concentration range within which maximum benefit is derived, and concentrations above or below this
range can be toxic or produce no therapeutic benefit at all. On the other hand, the very slow progress in the
efficacy of the treatment of severe diseases, has suggested a growing need for a multidisciplinary approach to
the delivery of therapeutics to targets in tissues. From this, new ideas on controlling the pharmacokinetics,
pharmacodynamics, non-specific toxicity, immunogenicity, biorecognition, and efficacy of drugs were
generated. These new strategies, often called drug delivery systems (DDS), are based on interdisciplinary
approaches that combine polymer science, pharmaceutics, bioconjugate chemistry, and molecular biology.

API Delivery

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To minimize drug degradation and loss, to prevent harmful side-effects and to increase drug bioavailability and
the fraction of the drug accumulated in the required zone, various drug delivery and drug targeting systems are
currently under development. Among drug carriers one can name soluble polymers, microparticles made of
insoluble or biodegradable natural and synthetic polymers, microcapsules, cells, cell ghosts, lipoproteins,
liposomes, and micelles. The carriers can be made slowly degradable, stimuli-reactive (e.g., pH- or
temperature-sensitive), and even targeted (e.g., by conjugating them with specific antibodies against certain

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characteristic components of the area of interest). Targeting is the ability to direct the drug-loaded system to
the site of interest. Two major mechanisms can be distinguished for addressing the desired sites for drug
release: (i) passive and (ii) active targeting. An example of passive targeting is the preferential accumulation of
chemotherapeutic agents in solid tumors as a result of the enhanced vascular permeability of tumor tissues
compared with healthy tissue. A strategy that could allow active targeting involves the surface
functionalization of drug carriers with ligands that are selectively recognized by receptors on the surface of the
cells of interest. Since ligandreceptor interactions can be highly selective, this could allow a more precise
targeting of the site of interest.
Controlled drug release and subsequent biodegradation are important for developing successful formulations.
Potential release mechanisms involve: (i) desorption of surface-bound /adsorbed drugs; (ii) diffusion through
the carrier matrix; (iii) diffusion (in the case of nanocapsules) through the carrier wall; (iv) carrier matrix
erosion; and (v) a combined erosion /diffusion process. The mode of delivery can be the difference between a
drugs success and failure, as the choice of a drug is often influenced by the way the medicine is administered.
Sustained (or continuous) release of a drug involves polymers that release the drug at a controlled rate due to
diffusion out of the polymer or by degradation of the polymer over time. Pulsatile release is often the preferred
method of drug delivery, as it closely mimics the way by which the body naturally produces hormones such as
insulin. It is achieved by using drug-carrying polymers that respond to specific stimuli (e.g., exposure to light,
changes in pH or temperature).
As a Novel

Up System

Drug Fact

Earth Novel

For over 20 years, researchers have appreciated the potential benefits of nanotechnology in providing vast
improvements in drug delivery and drug targeting. Improving delivery techniques that minimize toxicity and
improve efficacy offers great potential benefits to patients, and opens up new markets for pharmaceutical and
drug delivery companies. Other approaches to drug delivery are focused on crossing particular physical barriers,
such as the blood brain barrier, in order to better target the drug and improve its effectiveness; or on finding
alternative and acceptable routes for the delivery of protein drugs other than via the gastro-intestinal tract,
where degradation can occur.
1.1.1 Drug Delivery Carriers
Colloidal drug carrier systems such as micellar solutions, vesicle and liquid crystal dispersions, as well as
nanoparticle dispersions consisting of small particles of 10400 nm diameter show great promise as drug
delivery systems. When developing these formulations, the goal is to obtain systems with optimized drug
loading and release properties, long shelf-life and low toxicity. The incorporated drug participates in the
microstructure of the system, and may even influence it due to molecular interactions, especially if the drug
possesses amphiphilic and/or mesogenic properties.

ADMISSION

ADMISSION

Figure: 1 Pharmaceutical carriers

a) MICELLES:
Micelles formed by self-assembly of amphiphilic block copolymers (5-50 nm) in aqueous solutions are of great
interest for drug delivery applications. The drugs can be physically entrapped in the core of block copolymer
micelles and transported at concentrations that can exceed their intrinsic water- solubility. Moreover, the
hydrophilic blocks can form hydrogen bonds with the aqueous surroundings and form a tight shell around the
micellar core. As a result, the contents of the hydrophobic core are effectively protected against hydrolysis
and enzymatic degradation. In addition, the corona may prevent recognition by the reticuloendothelial system
and therefore preliminary elimination of the micelles from the bloodstream. A final feature that makes amphiphilic
block copolymers attractive for drug delivery applications is the fact that their chemical composition, total
molecular weight and block length ratios can be easily changed, which allows control of the size and
morphology of the micelles. Functionalization of block copolymers with crosslinkable groups can increase the
stability of the corresponding micelles and improve their temporal control. Substitution of block copolymer

ADMISSION

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micelles with specific ligands is a very promising strategy to a broader range of sites of activity with a much
higher selectivity.

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Figure: 2 Block copolymer micelles.

b) LIPOSOMES:
Liposomes are a form of vesicles that consist either of many, few or just one phospholipid bilayers. The polar
character of the liposomal core enables polar drug molecules to be encapsulated. Amphiphilic and lipophilic
molecules are solubilized within the phospholipid bilayer according to their affinity towards the phospholipids.
Participation of nonionic surfactants instead of phospholipids in the bilayer formation results in niosomes.
Channel proteins can be incorporated without loss of their activity within the hydrophobic domain of vesicle
membranes, acting as a size-selective filter, only allowing passive diffusion of small solutes such as ions,
nutrients and antibiotics. Thus, drugs that are encapsulated in a nanocage-functionalized with channel proteins
are effectively protected from premature degradation by proteolytic enzymes. The drug molecule, however, is
able to diffuse through the channel, driven by the concentration difference between the interior and the
exterior of the nanocage.

PYRRO LE, FU RA N ,
TH IO PH EN E
D ERIV A TIV ES &
PH A RM A C O LO GIC A L
A C TIV ITIES: A REV IEW
Rev iew o n: TH E
PH A RM A C EU TIC A L
PA C KA GIN G
M A N U FA C TU RIN G
D O C U M EN TA TIO N IN
PH A RM A C EU TIC A L
IN D U STRYD EV ELO PM EN T A N D
IM PLEM EN TA TIO N
FO RM U LA TIO N
D EV ELO PM EN T A N D
IN - V ITRO
EV A LU A TIO N O F
H YD RO PH ILLIC
M A TRIX BA SED
SA LBU TA M O L
SU LPH A TE TA BLETS
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D O C KIN G STU D IES O F
N - (2BEN Z O YLPH EN YL)- LTYRO SIN E
D ERIV A TIV ES W ITH
A N TI- D IA BETIC
A C TIV ITY O F TYPE 2
D IA BETES
REV IEW O N O C U LA R
D RU G D ELIV ERY

Figure: 3 Drug encapsulation in liposomes

c) DENDRIMERS:
Dendrimers are nanometer-sized, highly branched and monodisperse macromolecules with symmetrical
architecture. They consist of a central core, branching units and terminal functional groups. The core together
with the internal units, determine the environment of the nanocavities and consequently their solubilizing
properties, whereas the external groups the solubility and chemical behaviour of these polymers. Targeting
effectiveness is affected by attaching targeting ligands at the external surface of dendrimers, while their
stability and protection from the Mononuclear Phagocyte System (MPS) is being achieved by functionalization
of the dendrimers with polyethylene glycol chains (PEG).
d) LIQUID CRYSTALS:
Liquid Crystals combine the properties of both liquid and solid states. They can be made to form different
geometries, with alternative polar and non-polar layers (i.e., a lamellar phase) where aqueous drug solutions
can be included.
d) LIQUID CRYSTALS:
Liquid Crystals combine the properties of both liquid and solid states. They can be made to form different

FO RM U LA TIO N A N D
EV A LU A TIO N O F
A M O XIC ILLIN
TRIH YD RA TE
M O D IFIED RELEA SE
D O SA GE FO RM S
C O M PA RA TIV E
D ISSO LU TIO N
STU D IES FO R
A C EC LO FEN A C
M A RKETED D O SA GE
FO RM S
REGISTRA TIO N
D O SSIER O F
PH A RM A C EU TIC A LS

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geometries, with alternative polar and non-polar layers (i.e., a lamellar phase) where aqueous drug solutions
can be included.
e) NANOPARTICLES:
Nanoparticles (including nanospheres and nanocapsules of size 10-200 nm) are in the solid state and are either
amorphous or crystalline. They are able to adsorb and/or encapsulate a drug, thus protecting it against
chemical and enzymatic degradation. Nanocapsules are vesicular systems in which the drug is confined to a
cavity surrounded by a unique polymer membrane, while nanospheres are matrix systems in which the drug is
physically and uniformly dispersed. Nanoparticles as drug carriers can be formed from both biodegradable
polymers and non-biodegradable polymers. In recent years, biodegradable polymeric nanoparticles have
attracted considerable attention as potential drug delivery devices in view of their applications in the controlled
release of drugs, in targeting particular organs / tissues, as carriers of DNA in gene therapy, and in their ability
to deliver proteins, peptides and genes through the peroral route.
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