Abstract

A series of eight novel 2-Azetidinones (4a-h) have been synthesized by
cyclocondensation of various Schiff bases of 4-[(4-aminophenyl)amino]-
1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one with chloroacetyl
chloride in presences of triethylamine. Various Schiff bases were
synthesized by condensation of 4-[(4-aminophenyl)amino]-1,5-dimethyl-2-
phenyl-1,2-dihydro-3H-pyrazol-3-one with various arylaldehydes (3a-h).
The synthesized compounds (4a-h) were screened for their antibacterial
activity gainst six microorganisms: Staphylococcus aureus (Gram positive),
Bacillus subtilis (Grampositive), Salmonella typhi (Gram negative)
Escherichia coli (Gram negative) and fungal strain Aspergilius niger &
Candida Albicans. They were found to exhibit good to moderate
antibacterial activity. Among the eight derivative comp no-4e show the
good activity.The structures were confirmed by IR, 1H- NMR and Mass
spectral data.

Abstract

Cyanoacrylate and its derivatives attract the interesting investigative areas.
Cyanoacrylae molecule is generally described as macromolecule, which is
characterized by its extensive 3D structure that provides high degree of surface
functionality and versatility. The synthesis of cyanoacrylate polymer involves two
steps viz. double Michael addition step for formation of odd generation
cyanoarylate polymer and subsequent reduction of cyanoarylate polymer for
formation of even generation of cyanoacrylate polymer i.e. nitrile terminated
cyanoacrylate polymer. Of the two step, step number two i.e. reduction step is
highly crucial step in the scence that it involves many controlling parameters like
temperature, pressure, pH, and time of reaction. Considering the above fact, in the
present study an attempt was made to optimize the synthesis of cyanoacrylate
polymers. Further present study deals with gel formulation with cyanoacrylate
polymer and in vitro evaluation for the drug release. It has been found that
cyanoacrylate polymer helps to improve drug release by increasing binding of the
drug with receptor on cell membrane.

Atorvastatin Calcium is a lipid lowering drug. It is a HMG-CoA reductase
inhibitor used in the treatment of hyper lipidaemia. It has a oral
bioavailability of less than 12% Floating matrix tablets are designed to
prolong the gastric residence time after oral administration, at a particular
site and controlling the release of drug, especially useful for achieving
controlled plasma level as well as improving bioavailability. With this
objective, floating dosage form containing Atorvastatin Calcium as drug was
designed. Tablets containing hydroxypropylmethylcellulose (HPMC), drug
and different additives were compressed using wet granulation. The study
shows that tablet composition has great influence on the floating properties
and drug release. Incorporation of gas-generating agent together with
polymer improved drug release, besides optimal floating (floating lag time
~30 s; total floating time >12 h). The drug release was sufficiently sustained
(more than 11h) and non-Fickian as well as zero-order was confirmed.

The purpose of this research was to develop a matrix diffusion type transdermal
therapeutic system containing drug Lercanidipine with a blend of eudragit RL 100
and eudragit RS 100 as polymer system by the solvent evaporation technique
with PEG 400 as plasticizer. Glycerin was used as enhance the transdermal
permeation of Lercanidipine. Eight formulations with varied concentration of
polymers, plasticizers and permeation enhancers were done and optimization of the
concentration of formulation components was performed. Formulated transdermal
films were evaluated for various physicochemical parameters, in vitro release, and
stability studies. Good uniformity of the drug content among the patches was
observed for all the formulations which ranged from 94.75% to 98.42%.
Formulation variables such as polymer ratio, concentration of plasticizer and
permeation enhancers were found to influence the in vitro drug release behavior of
the formulated patches. Increasing the concentration of eudragit RL 100 and
plasticizer, the presence of permeation enhancers were found to increase the in
vitro drug release of the formulated patches. The total amount of drug released
from the films over 8 and 24 hours followed the order: 10% w/w Glycerin > 10%
w/w PEG 400 > 5% w/w Glycerin > 5 % w/w PEG 400. Based on the
physicochemical and drug release characteristics, the eudragit films with
polyethylene glycol 400 and glycerin are suitable to design matrix diffusion type
transdermal system for Lercanidipine and the F8 formulation with eudragit RL 100
to eudragit RS100 ratio 1:1, 5% w/w glycerin as permeation enhancer and 5% w/w
PEG 400 as plasticizer showed a thickness of 0.260mm and drug loading of
3.912mg/ cm2 was considered as the best formulation. The cumulative percentage
amount of drug release from the F8 formulation film was found to be 38.381% at
the end of 8 hours and 58.154% at the end of 24 hours. The films were found to be
stable during the entire stability period of 60 days at 45ºc.

Anti-inflammatory effects of Oxaprozin are believed to be due to inhibition of
cylooxygenase in platelets which leads to the blockage of prostaglandin synthesis.
Antipyretic effects may be due to action on the hypothalamus, resulting in an increased
peripheral blood flow, vasodilatation, and subsequent heat dissipation. The main objective
of this research work was to prepare HPMC microspheres loaded with Oxaprozin and invitro
drug release study. In the present study, emulsification-heat stabilizing method is used
for preparing microspheres. The polymer (HPMC) and drug (Oxaprozin) was dissolved in
deionsed water. Surfactant was added to this solution and stirred it for 30 min. The oil and
1% span-80 (as emulsifier) were mixed together and allowed to stir for 20 min at 800-1000
rpm. The aqueous phase was added to oil phase to form primary emulsion. This emulsion
were added to preheated sunflower oil and stirred for 3 hrs at 1000-1200 rpm. Microspheres
were filtered and dried in dessicator over night. Microspheres were spherical shape and
smooth surface. Infra-red spectra showed identical peaks of drug and polymer drug
entrapment efficiency was 69% determined by UV-Spectrophotometer at 267nm. In-vitro
drug release studies were preformed using shaking flask method. The formulation ZM1
Showed 87.5% drug was released in 10 hrs. It is concluded that HPMC microspheres of
Oxaprozin can be prepared by emulsification heat stabilizing method and in-vitro release
data is satisfactory.

Novel drug delivery system aims to provide some control in temporal
or spatial nature of the drug release in the body. In recent years,
vesicle have been the vehicle of choice in drug delivery for targeting
and controlled release and it can solve the problems of drug
solubility, instability and rapid degradation. Vesicular drug delivery
reduces cost of the therapy and can incorporate both the hydrophilic
and lipophilic drugs. Nowadays, a number of vesicular drug delivery
system such as liposome, pharmacosomes, ethosomes,
transferosomes etc. was developed. This article reviews different
aspects of this vesicular drug delivery system including their
preparation, characterization, advantages and their applications in the
drug delivery.