IAJPR

Indo American Journal of Pharmaceutical Research

ISSN NO.: 2231-6876
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May 2012
1

SLNs: An Overview, Preparation Techniques, Evaluations And Applications In Pharmacy

Patel Premda*, Sachin Chauhan, AK Seth
Department of Pharmacy, Sumandeep Vidyapeeth, Vadodara – 391760

Abstract

Current challenge to conventional drug delivery systems is to liberate a drug at
right time in a safe and reproducible manner to a specific targeted site. Targeted
delivery is one of the most important aspects of a drug delivery system to convey
the accurate and desired dose of the drugs and diagnostic agents to the specific
targeted site with the aid of suitable carriers.
The review aims majorly on four areas namely: Architecturing, Synthesis,
Properties & Applications of the solid lipid nanoparticles (SLNs). The unique
architectural design of SLNs like globular architecture and well-defined molecular
weight, clearly distinguishes these structures as unique and optimum nanocarriers
in medical applications such as drug delivery, gene transfection, tumor therapy,
diagnostics, etc. Synthetic approaches lead to architecture with properties
amenable to modifications of shape, size, polarity, surface properties and internal
structure. Nanoparticle drug-delivery systems are the popular ones as are able to
increase the selectivity and stability of therapeutic agents. However
reticuloendothelial system (RES) uptake, drug leakage, immunogenicity, hemolytic
toxicity, cytotoxicity, hydrophobicity restrict the use of these nanostructures. These
shortcomings are overcome by surface engineering the SLNs. The bioactive agents
can be easily encapsulated into the interior of the SLNs or chemically attached i.e.
conjugated or physically adsorbed onto the SLNs surface, serving the desired
properties of the carrier to the specific needs of the active material and its
therapeutic applications. In addition to supplying a multivalent backbone for drug
attachment, SLNs also provide access to various new polymer architectures that
are potentially relevant to drug delivery applications. This paper basically reviews
types of SLNs, principles of drug loading and models of drug incorporation. The
future direction of research and clinical implications of SLNs is also considered.

2

Recent Trends in Screening and Evaluation Methods of Anticancer Drugs

Rathod C.P *., Dhawale S.C., Kshirsagar R.V.
School of Pharmacy, S.R.T.M.U. Nanded

Abstract

Cancer is one of the major life threatening diseases worldwide. The available
anticancer drugs have distinct mechanisms of action which may vary in their effects on
different types of normal and cancer cells. Screening methods are routinely and extensively
used to reduce cost and time of drug discovery. The traditional anticancer drug screening
methods, including animal experiments and cell-based screening assays. Screening methods
for the detection of anticancer activity are of importance in order to find solid tumorspecific
agents. The screening and evaluation procedures for the development of anticancer
agents indicated that the entire process is a rather difficult task. Presently, active
compounds are selected by prescreening and screening against transplanted mouse tumors
and human tumor xenografts as well as by the in vitro systems. The US National Cancer
Institute (NCI) 60 human tumour cell line anticancer drug screen (NCI60) was developed in
the late 1980s as an in vitro drug-discovery tool intended to supplant the use of
transplantable animal tumours in anticancer drug screening. This screening model give
information about the mechanisms of growth inhibition and tumour-cell kill. Recently, its
role has changed to that of a service screen supporting the cancer research community.
Target-based and cell-based screenings for new anticancer drugs in the molecular targeting
period are methods of identifying more selective anticancer drugs. Here I review the
development, use and productivity of the screen, highlighting several outcomes that have
contributed to advances in cancer chemotherapy. Finally, we discuss primary and secondary
in vivo evaluation in experimental chemotherapy.

3

GASTRORETENTIVE MUCOADHESIVE MICROSPHERE: A REVIEW

Madhav S. Mule1,Mr. Kshirsagar R.V.*
1School of Pharmacy, S.R.T.M.U. Nanded,

Abstract

The current article focuses on the principles of mucoadhesive drug delivery systems based
on adhesion to biological surfaces that are covered by mucus. In recent years scientific and
technological advancements have been made in the research and development of
Mucoadhesive Microsphere by overcoming physiological adversities like short gastric
residence times and unpredictable gastric emptying times. Gastroretentive drug delivery
systems are the systems which are retained in the stomach for a longer period of time and
thereby improve the bioavailability of drugs. Different approaches for Gastroretentive
dosage forms include floating, expanding or swelling, bioadhesive or mucoadhesive and
high/low-density systems. The Mucoadhesive Microsphere should be primarily aimed to
achieving more predictable and increased bioavailability of drugs. Prolonged gastric
retention improves bioavailability, reduces drug waste, useful for drugs acting locally in the
GIT, drugs which are poorly soluble and unstable in intestinal fluids. These systems are
advantageous in improving GIT absorption of drug with CR due to specific site absorption
limitations. By using mucoadhesive hydrogels as drug carriers is given. Techniques that are
frequently used to study the adhesion forces and physicochemical interactions between
hydrogel, mucus, and the underlying mucosa are reviewed. Typical examples of
applications of mucoadhesive hydrogels to mucosal routes of delivery are given. Various
methods of preparation, evaluation test, application. Factors affecting, polymer used and
mechanism of bioadhesion are discussed here. Mucoadhesive drug delivery systems is one
of the most important novel drug delivery systems with its various advantages and it has a
lot of potential in formulating dosage forms for various chronic diseases.

4

Formulation, Development and Characterization of Oral Disintegraing Tablet of Ranitidine HCl

Samar Doshi, Gajanan Deshmukh and Dr. A. K. Seth.
Department of Pharmacy, Sumandeep Vidyapeeth, Vadodara, Gujarat, India.

Abstract

Ranitidine HCl is a recognized drug for peptic ulcer therefore development of an ODT of Ranitidine HCl and to evaluate the effect of various
superdisintegrants on its disintegration time and release profile was the prime objective of this research work. Tablets were prepared by direct
compression technique using 3 different superdisintegrants. Sodium starch glycolate, Croscarmellose sodium and Crosspovidone XL-10 were used as superdisintegrants in combinations and individually to achieve optimum release profile, disintegration time and hardness. Direct compression process was selected for this formulation of ODT tablets, because porous nature is more in direct compression blend than wet granulation blend, so it will give faster disintegration. Microcrystalline cellulose was used as diluent and mannitol, mint flavor and sodium saccharin were used to enhance the
organoleptic properties of tablets. The tablets were evaluated for weight variation, hardness, friability, in-vitro disintegration time and drug release
characteristics. Hardness and friability data indicated good mechanical strength around 3 kg/cm2 for all the batches. The results of in-vitro
disintegration time indicated that the tablets dispersed rapidly in mouth within 30s. It was concluded that superdisintegrants addition technique is a
useful method for preparing orally disintegrating tablets by direct compression method.

5

Formulation and Evaluation of Telmisartan Microspheres by Solvent Evaporation Technique

Prakash N. Kendre*, Pravin D. Chaudhari1
*Dept. of Pharmaceutics, Sanjivani College of Pharmaceutical Education & Research, Kopargaon, Dist.Ahmednagar (M.S.), India-423 603
1Dept. of Pharmaceutics,Modern College of Pharmacy, Nigadi, Pune

Abstract

Microspheres, a multi-component system which provides constant
and prolonged drug release. Furthermore their floating abilities
increase gastric residence time. These properties reduce the
gastrointestinal toxic effects and dosing frequency and thereby
improve the patient compliance. The present study aimed to
formulate and evaluate Telmisartan microspheres. Emulsion solvent
evaporation technique was employed for microspheres preparation
using different ratios of ethyl cellulose and drug. Prepared
microspheres were evaluated for drug entrapment efficiency,
micromeritic characteristics, floating behaviour and in vitro drug
release. This study revealed that varying concentrations of polymer
has significant influence on drug release.

6

Pharmacodynamic Studies of Lercanidipine hydrochloride Transdermal Therapeutic Systems

Subhash P.G.*1, Dinesh B.M.2, Ravikumar M.3
1East West College of Pharmacy, B.E.L. Layout, Magadi Road, Vishwaneedam Post, Bangalore -560091, Karnataka, India.
2KLE University's College of Pharmacy, II Block, Rajajinagar, Bangalore -560010, Karnataka State, India.
3Geethanjali College of Pharmacy, Cheeryala (V), Keesara (M), Rangareddy Dist., A.P,50101, India.

Abstract

This article reports the assessment of lercanidipine hydrochloride (LH) for transdermal
delivery. In-vitro permeation studies were carried out across the porcine ear skin in presence
of various penetration enhancers. Pharmaceutical excipients and chemicals namely dimethyl
sulfoxide (DMSO), isopropyl myristate (IPM), sodium lauryl sulphate (SLS), eugenol,
citral, hyaluronidase were facilitated to evaluate as effective penetration enhancer. Among
all, hyaluronidase emerged as effective penetration enhancer with highest flux 111.8±0.030
μg/cm2/hr, Kp 0.0172±0.040 cm/hr and enhancement ratio 5.37±0.01 than others. Later, LH
(10 mg/3.14 cm2) transdermal patches (designated as EL formulations) were prepared by
using EC and PVP K-30 as polymers in 1:2 ratio incorporating optimized hyaluronidase (5%
w/w) as penetration enhancer, n - dibutyl phthalate (30% w/w) as a plasticizer. The ex-vivo
permeation studies of EL formulations exhibited satisfactory cumulative percent of drug
permeation, transdermal flux, permeability coefficient and diffusion coefficient. The curve
fitment data indicated that the in-vitro permeation data of model formulations fitted well
into zero order equation (average R2=0.9713 to 0.9866) better than first order and Higuchi
model. The pharmacodynamic studies were carried out employing rat tail cuff method in
albino rats. Hypertension was successfully induced by methyl prednisolone acetate (MPA)
(40 mg/kg) subcutaneously for 2 weeks. The fabricated EL transdermal patches were
significantly decreased the blood pressure (BP) in close to normal values for 24 hours.
Furthermore, the satisfactory results were supported by one way ANOVA.

7

ETHOSOMAL DRUG DELIVERY SYSTEM: A REVIEW

N.B.MAHALE*, S.A. KHAIRNAR, R.N.KANAWADE, K.K.WALE, D.D. NAVANDAR S.R.CHAUDHARI.
Department of Pharmaceutics, Amrutvahini College of Pharmacy, Amrutnagar, Sangamner- 422608,Dist.
Ahmednagar, Maharashtra, India.

Abstract

The vesicles have been well known for their important in cellular
communication and particle transportation for many years. Researchers have
understood the properties of vesicle structures for use in better drug delivery within
their cavities, that would allow to tag the vesicle for cell specificity. Vesicles would
also allow to control the release rate of drug over an extended time, keeping the
drug shielded from immune response or other removal systems and would be able
to release just the right amount of drug and keep that concentration constant for
longer periods of time. One of the major advances in vesicle research was the
finding a vesicle derivative, known as an ethosomes. Ethosomes are modified lipid
carriers that enable drugs to reach into deeper skin layers and/or systemic
circulation, and represent a lipid vesicular carrier system embodying ethanol in
relatively high concentration and are very effective in delivering drugs into and
across the skin.

8

SOLUBILITY ENHANCEMENT OF AMISULPRIDE BY SOLID DISPERSION TECHNIQUE AND PREPARATION OF FAST DISSOLVING TABLETS

Murali Krishna. T*, Vivek Kumar A. Patel, RajashekarValluru, Dr. Jagadeesh G. Hiremath, Prathapreddy .D
Dept of pharmaceutics, East West College of Pharmacy, B.E.L. Layout, 63, Magadi Road Viswaneedam Post Bangalore-560091, Karnataka, India.

Abstract

Amisulpride exhibits anti-psychotic activities by selectively binding to
dopamine D(2) and D(3) receptors in the limbic system. It is used in the
treatment of psychoses, paranoid, productive schizophrenias, dysthymia.
However, amisulpride (AMP) is poorly water soluble drug, so solubility is
the main constraint for oral bioavailability. An attempt has been made to
increase the solubility of this drug by formulating solid dispersion (SD) by
using β-cyclodextrin (β-CD) employing spray drying method and then
formulating fast dissolving tablets(FDT). Among the two different
formulation of SD, formulation SD2 containing amisulpride & β-CD in the
ratio of 1:2 gives best drug content and dissolution profile and among tablet
formulations. FDTs were prepared by direct compression technique using
superdisintegrants such as croscarmellose sodium and sodium starch
glycolate in different concentrations. SDs were characterized by FT-IR,
DSC analysis and evaluated for drug content and in vitro dissolution
profiles. Tablet formulations were evaluated for pre compressional
parameters such as angle of repose, bulk & tap density, Carr’s index,
Hausner’s ratio and post compression parameters such as hardness,
friability, weight variations, drug content, wetting time, disintegration time
and in vitro dissolution profile. Formulation CF2 containing 6.5%
croscarmellose sodium gives best disintegration and dissolution profile
compared with other formulations. Results showed that β-cyclodextrin is a
promising polymer for enhancing the solubility of AMP