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Current
Drug Delivery
ISSN: 1567-2018
Current Drug Delivery
Volume 6, Number 1, January 2009
Contents
Aceclofenac Organogels: In Vitro and In Vivo
Characterization Pp. 1-7
I.M. Shaikh, S.L. Jadhav, K.R. Jadhav, V.J. Kadam
and S.S. Pisal
[Abstract] [Full
Text Article]
Aerosol Performance of Large Respirable Particles
of Amikacin Sulfate Produced by Spray and Freeze Drying TechniquesPp.
8-16
Bijay K. Padhi, Mahavir B. Chougule
and Ambikanandan Misra
[Abstract] [Full
Text Article]
Fluconazole Mucoadhesive Buccal Films: In Vitro/In
Vivo PerformancePp. 17-27
Soad A. Yehia, Omaima N. El-Gazayerly and
Emad B. Basalious
[Abstract] [Full
Text Article]
Design, Optimization, Preparation and Evaluation of
Dispersion Granules of Valsartan and Formulation into TabletsPp.
28-37
Agnivesh R. Shrivastava, Bhalchandra Ursekar
and Chhanda J. Kapadia
[Abstract] [Full
Text Article]
Aerosol Devices and Asthma TherapyPp. 38-49
William Berger
[Abstract] [Full
Text Article]
Design and Evaluation of a Bioadhesive Patch for Topical
Delivery of Gentamicin SulphatePp. 50-57
N.A. El-Gendy, G.A. Abdelbary, M.H. EL-Komy
and A.E. Saafan
[Abstract] [Full
Text Article]
Efficacy of Pegylated Lyposomal Anthracyclines and
of Intra Arterial Carboplatin and Doxorubicin Combined with
Local Hyperthermia in a Case of Malignant Endovascular Papillary
AngioendotheliomaPp. 58-61
Amedeo Fiorillo, Gaetano DeRosa, Francesca
Giugliano, M. Laura DeLillo, M. Simona Sabbatino and
Antonella Veneziano
[Abstract] [Full
Text Article]
Poly (D, L-Lactide) Nanosuspensions of Risperidone
for Parenteral Delivery: Formulation and In-Vitro EvaluationPp.
62-68
M.S. Muthu and S. Singh
[Abstract] [Full
Text Article]
Preparation and Characterization of Cephalexin Loaded
PLGA MicrospheresPp. 69-75
Wasana Chaisri, Wim E. Hennink and
Siriporn Okonogi
[Abstract] [Full
Text Article]
Enhancement of Immunoprotective Effect of CpG-ODN
by Formulation with Polyphosphazenes Against E. coli
Septicemia in Neonatal Chickens Pp. 76-82
Azita Taghavi, Brenda Allan, George Mutwiri,
Marianna Foldvari, Andrew Van Kessel, Philip Willson, Lorne
Babiuk , Andrew Potter and Susantha Gomis
[Abstract] [Full
Text Article]
Rheological Properties of Vaginal Hydrophilic Polymer
GelsPp. 83-92
José das Neves, Marta Vázquez
da Silva, Maria Pilar Gonçalves, Maria Helena Amaral
and Maria Fernanda Bahia
[Abstract] [Full
Text Article]
Effect of Vehicle on Diclofenac Sodium Permeation
from New Topical Formulations: In Vitro and In
Vivo StudiesPp. 93-100
Vanna Sanna, Alessandra T. Peana and
Mario D.L. Moretti
[Abstract] [Full
Text Article]
Improvement in Chemical and Physical Stability of
Fluvastatin Drug Through Hydrogen Bonding Interactions with
Different Polymer MatricesPp. 101-112
G.Z. Papageorgiou, S. Papadimitriou, E.
Karavas, E. Georgarakis, A. Docoslis and D. Bikiaris
[Abstract] [Full
Text Article]
Formulation and Evaluation of Oral Mucoadhesive Multiparticulate
System Containing Metoprolol Tartarate: An In Vitro –
Ex Vivo CharacterizationPp. 113-121
Veena Belgamwar, Viral Shah and S.J.
Surana
[Abstract] [Full
Text Article]
Recent Advances in Pelletization Technique for Oral
Drug Delivery: A ReviewPp. 122-129
Md. Akhlaquer Rahman, Alka Ahuja, S. Baboota,
Bhavna, Vikas Bali, Nitin Saigal and Javed Ali
[Abstract] [Full
Text Article]
Development and Evaluation of Elementary Osmotic Pump
of Highly Water Soluble Drug: Tramadol HydrochloridePp.
130-139
Pramod Kumar, Sanjay Singh and
Brahmeshwar Mishra
[Abstract] [Full
Text Article]
Development and Characterization of Mucoadhesive Buccal
Patches of Salbutamol SulphatePp. 140-144
Rajesh Singh Patel and S.S. Poddar
[Abstract] [Full
Text Article]
Abstracts
[Back to top]
Aceclofenac Organogels: In Vitro and
In Vivo Characterization
I.M. Shaikh, S.L. Jadhav, K.R. Jadhav, V.J. Kadam
and S.S. Pisal
[Full
Text Article]
Purpose: To develop and evaluate
the suitability of lecithin organogels containing aceclofenac
for topical application and compare its In vitro
and In vivo effects with conventionally used hydrogels.
Methods: The components and their concentration
necessary for organogels formation were evaluated using phase
diagram. Solubility of aceclofenac was determined. The In
vitro skin permeation ability of aceclofenac from ethyl
oleate based lecithin organogels [EO/lecithin organogel] and
hydrogel was investigated. The In vivo characterization
of ethyl oleate based organogel study was compared with that
of hydrogel.The alterations in microstructure of organogels
during diffusion study were elucidated. Viscosity and micellar
size of the organogel sample were estimated. The safety of
optimized organogel was determined using histopathological
investigation.
Results: The flux calculated for
skin permeation ability of aceclofenac was in the order EO/lecithin
organogel >
hydrogel.The In vivo results also demonstrated that
organogels are more effective in faster drug release as compared
to hydrogels. It was observed that viscosity of gels decreased
with increasing stress .The size of micellar aggregation increased
with water added and has been revealed in dynamic light scattering
(DLS) study. The histopathological data showed that EO/lecithin
organogel were safe enough for topical purpose.
[Back to top]
Aerosol Performance of Large Respirable Particles
of Amikacin Sulfate Produced by Spray and Freeze Drying Techniques
Bijay K. Padhi, Mahavir B. Chougule
and Ambikanandan Misra
[Full
Text Article]
The purpose of the present study was to investigate the
influence of method of preparation of large respirable particles
of amikacin sulphate on traits and topography and in-vitro
aerosol performance. Large respirable particles of amikacin
sulfate (50%w/w) were produced by spray-drying and freeze-drying
processes using hydrogenated soyaphos-phatidylcholine, L-leucine
and Poloxamer 188. Particles exhibited 0.04–0.08 g/cm3
tap densities, 7-20 μm
geometric particle size, and 1 to 5 µm of mean aerodynamic
diameter. Apart from the morphology and topographical features,
spray-dried and freeze- dried particles had marginal difference
in their solid-state characteristics. Spray-dried particles
were dimpled spherical shape with roundness value close to
1(1.066 ±
0.028), relatively smooth surface texture and produced greater
aerosol dispersion with 20% higher fine particle fraction,
6.92% lower impaction loss and 13% less capsule and device
retention than freeze dried particles. Traits and topographical
features, such as particle size, polydispersity, elongation
ratio, roundness, shape, and degree of surface roughness were
found to be influenced significantly by spray-drying process
and particles produced by spray-drying process showed better
aerosol performance due to these differences.
[Back to top]
Fluconazole Mucoadhesive Buccal Films: In Vitro/In
Vivo Performance
Soad A. Yehia, Omaima N. El-Gazayerly and
Emad B. Basalious
[Full
Text Article]
Fluconazole mucoadhesive buccal films were prepared using
film forming polymers namely; hydroxypropyl methyl cellulose
(HPMC), hydroxyethyl cellulose (HEC), chitosan, Eudragit and
sodium alginate (SALG) either alone or in combination with
bioadhesive polymers. The bioadhesive polymers studied were
sodium carboxymethyl cellulose (SCMC), Carbopol 974P, and
polycarbophil (AA-A). The prepared films were characterized
by means of film thickness, surface pH, swelling capacity,
in vitro adhesion, in vivo residence time,
in vitro drug release and in vivo drug release
to determine the amount of drug release from selected film
formulae using microbiological assay and HPLC. Optimum release
behavior, convenient bioadhesion, acceptable elasticity were
exhibited by film containing 2% HPMC and 1% SCMC (fresh or
stored for 6 months). Determination of the amount of drug
released in saliva after application of the selected fluconazole
films confirmed the ability of the film to deliver the drug
over a period of approximately 300 minutes and to reduce side
effects and possibility of drug interaction encountered during
systemic therapy of fluconazole, which would be beneficial
in the case of oral candidiasis.
[Back to top]
Design, Optimization, Preparation and Evaluation of
Dispersion Granules of Valsartan and Formulation into Tablets
Agnivesh R. Shrivastava, Bhalchandra Ursekar
and Chhanda J. Kapadia
[Full
Text Article]
The objective of the present work undertaken was to enhance
the solubility and dissolution rate of valsartan a poorly
water soluble antihypertensive, by preparation of solid dispersion
granules which would additionally allow easy compression into
tablets. The dispersion granules were prepared using a hot
melt granulation technique which involved preparation of a
homogenous dispersion of valsartan in gelucire-50/13 melt,
followed by its adsorption on to the surface of aeroperl-300pharma®
an inert adsorbent. A two-factor, three-level (32)
statistical design was implemented to quantitate the influence
of gelucire-50/13 and aeroperl-300pharma on the dissolution
profile and flow properties of the dispersion granules, where
gelucire-50/13 and aeroperl-300pharma®
were chosen as independent variables, while dissolution and
flow properties were chosen as dependent variables. The dispersion
granules were characterized for their in-vitro dissolution
rate and flow properties. An appropriate statistical model
was arrived at and a significantly enhanced dissolution rate
and flow properties were exhibited with the optimized formulation.
The formulation was further characterized by FTIR, DSC, XRD
and SEM analysis. FTIR spectrum revealed some drug excipient
interactions. DSC and XRD data indicated the retention of
amorphous form of valsartan. SEM confirmed the homogeneity
and surface adsorption of the gelucire-50/13 melt on aeroperl-300pharma®
leading to enhanced surface area and thus dissolution rate.
The tablets of optimized dispersion granules were formulated
and evaluated. The in-vitro dissolution rate of these
tablets was significantly better in comparison with marketed
formulation. In conclusion the statistical model enabled us
to understand the effects of formulation variables on the
dispersion granules of valsartan.
[Back to top]
Aerosol Devices and Asthma Therapy
William Berger
[Full
Text Article]
Aerosol delivery of asthma medications maximizes local
effects in the lung and minimizes systemic effects compared
with oral therapy. Both corticosteroids and bronchodilators
are available in a variety of delivery devices for the treatment
of asthma. The 1987 Montreal protocol requiring the phasing
out of the chlorofluorocarbon (CFC) propellant in commonly
used pressurized metered-dose inhalers (pMDIs) provided an
impetus for the development of new technologies for the delivery
of inhaled asthma medications. For pMDIs, CFC has been replaced
with hydrofluoroalkane (HFA) pro-pellant. New types of dry
powder inhalers (DPIs) and nebulizers, aerosol delivery devices
that do not use propellants, also have been introduced. Drug
delivery varies based on the device type, the product formulation
and patient-related factors. Thus, drug delivery can differ
when the same medication is delivered via an HFA pMDI, a CFC
pMDI, a DPI or a nebulizer. Even among the same type of device
(eg. DPIs, pMDIs), inhaler designs and drug formulations differ.
Drug and device selection should be based on consideration
of the patient’s ability to use the device properly,
the availability of a desired drug or drugs (ie. maintenance
and rescue) in a particular inhaler device and patient preference.
This review describes key characteristics for each device
type, explains differences in markers of lung deposition,
lists potential advantages and disadvantages of the different
devices and discusses how these and other factors need to
be considered when selecting an inhaler device that meets
the individual needs of a patient.
[Back to top]
Design and Evaluation of a Bioadhesive Patch for Topical
Delivery of Gentamicin Sulphate
N.A. El-Gendy, G.A. Abdelbary, M.H. EL-Komy
and A.E. Saafan
[Full
Text Article]
The use of aminoglycoside antibiotics for the topical
treatment of gram positive and gram negative infections especially
burns and wounds has increased markedly in recent years. Patch
formulation for topical delivery can be advantageously used
as an alternative to conventional topical dosage forms. The
present study aims to prepare and evaluate gentamicin sulphate
patches for topical application and to study the effect of
different bioadhesive polymers on diverse characteristics
of prepared patches. Drug patches were evaluated for weight
and thickness uniformity, moisture absorption capacity, tensile
strength and percentage elongation. In vitro release
patterns of these patches were studied and analyzed. Skin
irritation and susceptibility testing of gentamicin sulphate
formulae were also evaluated and compared to commercially
available gentamicin sulphate cream. The thickness of the
films was found to be uniform. Tensile strength of the patches
prepared using HPMC as bioadhesive polymer was the lowest
compared to the other patches. The in vitro release
of the patches followed a pattern close to diffusion model.
Patches formulated using HPMC gave the most superior results
as compared to other compositions.
[Back to top]
Efficacy of Pegylated Lyposomal Anthracyclines and
of Intra Arterial Carboplatin and Doxorubicin Combined with
Local Hyperthermia in a Case of Malignant Endovascular Papillary
Angioendothelioma
Amedeo Fiorillo, Gaetano DeRosa, Francesca
Giugliano, M. Laura DeLillo, M. Simona Sabbatino and
Antonella Veneziano
[Full
Text Article]
Malignant vascular tumors are exceedingly rare in childhood.
Generally, their prognosis is dependent from a microscopically
complete surgical resection. We observed the case of a 4-year-old
boy affected by malignant endovascular papillary angioendothelioma,
a rare vascular tumor of intermediate malignancy, involving
all his left leg and partially the pelvis. Its very large
size hampered any surgical intervention. However, we could
demonstrate high sensitivity of the tumor to lyposomal anthracyclines
and the child was eventually cured by the intra-arterial administration
of carboplatin and doxorubicin coupled with local hyperthermia.
This experience probably represents the first step toward
an effective treat-ment of malignant vascular tumors in infancy.
[Back to top]
Poly (D, L-Lactide) Nanosuspensions of Risperidone
for Parenteral Delivery: Formulation and In-Vitro Evaluation
M.S. Muthu and S. Singh
[Full
Text Article]
Risperidone, an “atypical” antipsychotic
drug, having large scope for prolonged psychotic treatments
through novel parenteral drug delivery systems. Polymeric
nanoparticles suspensions containing risperidone made of poly
(D, L-Lactide) were designed by nanoprecipitation method using
polymeric stabilizer (Pluronic®
F-68 or Pluronic®
F-127). The prepared nanosuspensions were characterized for
particle size by photon correlation spectroscopy and scanning
electron microscopy. The free dissolved drug in the nanosuspension
was determined by bulk equilibrium reverse dialysis bag tech-nique.
In vitro release studies were carried out using dialysis
bag diffusion technique. The particle size of the prepared
nanoparticles in the nanosuspensions ranged between 78-184
nm. Nanoparticles of risperidone in the nanosuspensions were
obtained with high encapsulation efficiency (91 - 94 %). The
drug release from the risperidone nanosuspension was sustained
in some batches for more than 24 h with 75% drug release whereas
release from risperidone solution showed release within 1.5
h. The release pattern of drug is analyzed and found to follow
first order equation and Fickian diffusion kinetics. These
studies suggest the feasibility of formulating risperidone
loaded poly (D, L-Lactide) nanoparticles suspension for the
treatment of psychotic disorders.
[Back to top]
Preparation and Characterization of Cephalexin Loaded
PLGA Microspheres
Wasana Chaisri, Wim E. Hennink and
Siriporn Okonogi
[Full
Text Article]
The aim of this study was to evaluate the effects of
emulsion type and process parameters on the properties of
CPX-loaded PLGA microspheres in order to obtain delivery systems
suitable for the treatment of dairy mastitis. The microsphere
size was analyzed by photon correlation spectrophotometry.
Determination of the drug loading was achieved by HPLC. It
was found that CPX-loaded PLGA microspheres prepared using
a w/o/w double emulsion technology were slightly larger (~
3-5 μm)
but much higher in drug content (~ 18 % w/w) than those obtained
using o/w single emulsion preparation technology (average
size was 2 μm,
encapsulation efficiency was less than 2 %). It was also demonstrated
that stirring during emulsification and a change in both the
internal and external phase of the emulsion, affected the
size and the drug entrapment efficiency of the microspheres
obtained. A 60/40 v/v mixture of chloroform and acetone was
found to be the best organic solvent system for creating the
primary emulsion. To obtain a high yield (>90%)
of microspheres with a desirable size and high drug entrapment
efficacy, a stirring rate of 8,000-10,000 rpm gave the best
results. It is concluded CPX-loaded PLGA microspheres with
suitable characteristics for the treatment of cows with dairy
mastitis can be prepared by a w/o/w double emulsion preparation
method.
[Back to top]
Enhancement of Immunoprotective Effect of CpG-ODN
by Formulation with Polyphosphazenes Against E. coli
Septicemia in Neonatal Chickens
Azita Taghavi, Brenda Allan, George Mutwiri,
Marianna Foldvari, Andrew Van Kessel, Philip Willson, Lorne
Babiuk , Andrew Potter and Susantha Gomis
[Full
Text Article]
Synthetic oligodeoxynucleotides (ODN) containing CpG
motifs (CpG-ODN) have been shown to be effective immunoprotective
agents and vaccine adjuvants in a variety of bacterial and
protozoan diseases in different animal species. The objective
of this study was to investigate the immunoprotective effect
of formulated CpG-ODN with polyphos-phazene, liposome or oil-in-water
emulsion against E. coli infections in neonatal chickens.
Eighteen-day-old embryonating eggs were inoculated with 50
μg
CpG-ODN or formulated CpG-ODN with polyphophazene, liposome
or oil-in-water emulsion. Four days after exposure to formulated
CpG-ODN or day-1 post-hatch, 1x104
or 1x105 cfu of a virulent
isolate of E. coli was inoculated by the subcutaneous
route in the neck. Clinical signs, pathology, bacterial isolations
from the air sacs, and mortality were observed for eight days
following challenge with E. coli. The survival rate
of birds following E. coli infection was 0% in groups
receiving either non-CpG-ODN or saline. In contrast, birds
receiving either CpG-ODN or CpG-ODN formulated with polyphosphazene
had significantly higher survival of 55% (P<0.0001).
The relative risk of mortality was significantly reduced for
birds treated with CpG-ODN formulated in PCPP (0.25), in PCEP
(0.33), or unformulated CpG-ODN (0.39) in comparison to the
group treated with saline (p<0.01).
Although formulation of CpG-ODN with liposomes or oil-in-water
emulsion did not increase the immunoprotective effect against
E. coli infection, no adverse reactions or poor hatchability
were observed in embryos. This is the first time that CpG-ODN
formulated with polyphos-phazene has been demonstrated to
have an immunoprotective effect against an extra cellular
bacterial infection in neonatal broiler chickens following
in ovo delivery.
[Back to top]
Rheological Properties of Vaginal Hydrophilic Polymer
Gels
José das Neves, Marta Vázquez
da Silva, Maria Pilar Gonçalves, Maria Helena Amaral
and Maria Fernanda Bahia
[Full
Text Article]
The objective of this work was to investigate the main
rheological features of vaginal hydrophilic polymer gels and
to elucidate about the relationship between these characteristics
and gels composition, and their general influence in therapeutic/usage
purpose. Flow and dynamic oscillatory properties of four commercially
available (Conceptrol®,
Gynol II®,
RepHresh®,
and Replens®)
and two investigational vaginal gels were determined by cone-and-plate
rheometry, at body temperature. Several parameters (apparent
viscosity, complex viscosity, storage modulus, loss modulus,
critical oscillatory stress, tan δ,
thixotropy and yield stress) were measured and/or calculated.
Gels presented non-Newtonian, pseudoplastic, thixotropic behavior,
with yield stress. Overall viscosities varied between 13500
Pa.s and approximately 80 Pa.s within a biologically relevant
shear rate interval (0.01-100 s-1).
Yield stress values were variable between different determination
methods but coherent in terms of ranking. Also, tested gels
showed viscoelastic properties, being characterized by predominant
elastic solid-like behavior. Rheological behavior of vaginal
gels strongly depended on the type of gelling agent used,
which potentially influences their spreading and retention
properties when administered in the vaginal canal. Small variations
in gels composition can result in substantial changes in their
features, namely viscosity, yield stress and thixotropy. Rheological
properties of tested gels appeared to be correlated with their
therapeutic/usage purpose.
[Back to top]
Effect of Vehicle on Diclofenac Sodium Permeation
from New Topical Formulations: In Vitro and In
Vivo Studies
Vanna Sanna, Alessandra T. Peana and
Mario D.L. Moretti
[Full
Text Article]
In this study the effect of vehicle on in vitro
diffusion of diclofenac sodium (DS) from new different formulations
such as Carbopol gel (A), Sodium lauryl sulphate cream (B)
and Carbopol cream (C) was evaluated with Franz diffusion
cells using hydrophilic and hydrophobic synthetic membranes.
The commercial formulation Voltaren®
Emulgel was used as reference.
Furthermore, the in vivo efficacy of topical formulations
was studied in the carrageenan-induced edema and hyperalgesia,
whereas the antinociceptive effect was evaluated on thermal
pain threshold in rat paw.
The flux of DS across hydrophilic membranes showed this rank
order: Control ≈
C >
A ≈
B. On the other hand, the diffusion rate of DS across hydrophobic
membranes resulted in the following order: Control >
B >
A ≈
C; this suggested a lower interaction between the vehicles
and these membranes.
The in vivo results indicated that the prepared formulations
failed in the inflammatory tests to reduce the development
of edema.
Nevertheless, treatment with B formulation inhibited the development
of acute hyperalgesia induced by carrageenan, and elicited
a significant increase in paw withdrawal latencies whereas
other formulations were ineffective.
The results obtained in this study suggest that Sodium lauryl
sulphate cream might be useful in local pain conditions and
may be an effective alternative to the presently used systemic
routes.
[Back to top]
Improvement in Chemical and Physical Stability of
Fluvastatin Drug Through Hydrogen Bonding Interactions with
Different Polymer Matrices
G.Z. Papageorgiou, S. Papadimitriou, E.
Karavas, E. Georgarakis, A. Docoslis and D. Bikiaris
[Full
Text Article]
Solid dispersions of Fluvastatin with polyvinylpyrrolidone
(PVP), eudragit RS100 (Eud), and chitosan (CS) as drug carrier
matrices, were prepared using different techniques in order
to evaluate their effect on Fluvastatin stability during storage.
The characterization of the three different systems was performed
with the use of differential scanning calorimetry (DSC) and
wide angle X-ray diffractometry (WAXD). It was revealed that
amorphization of the drug occurred in all of the solid dispersions
of Fluvastatin as a result of drug dissolution into polymer
matrices and due to physical interactions (hydrogen bonding)
between the polymer matrix and Fluvastatin. This was established
through the use of FTIR spectroscopy. SEM and micro-Raman
spectroscopy showed that Fluvastatin was interspersed to the
polymer matrices in the form of molecular dispersion and nanodispersion,
too. The finding that completely different polymer matrices,
used here as drug carriers, produce completely different dissolution
profiles for each one of the solid dispersions, suggests that
each matrix follows a different drug release mechanism. Hydrogen
bonding interactions as in the case of CS/Fluva solid dispersions
lead to controlled release profiles. All formulations were
subjected to accelerated aging in order to evaluate Fluvastatin
stability. From by-products analysis it was found that Fluvastatin
is very unstable during storage and anti-isomer as well as
lactones are the main formed by-products. On the other hand,
solid dispersions due to the evolved interactions of their
reactive groups with Fluvastatin provide a sufficient physical
and chemical stability. The extent of interactions seems to
play the most important role in the drug stabilization.
[Back to top]
Formulation and Evaluation of Oral Mucoadhesive Multiparticulate
System Containing Metoprolol Tartarate: An In Vitro –
Ex Vivo Characterization
Veena Belgamwar, Viral Shah and S.J.
Surana
[Full
Text Article]
The aim of the present study was to prepare mucoadhesive
multiparticulate system for oral drug delivery using ionic
gelation technique. Microspheres composed of various mucoadhesive
polymers including HPMC of various grades like K4M, K15M,
K100M, E50LV, Carbopol of grades 971P, 974P and polycarbophil
were prepared. In this technique cross linking of sodium alginate
with calcium chloride was done which retarded the release
of drug from the mucoadhesive polymer. In the present work
Metoprolol tararate was used as a model drug. Interaction
studies performed using FTIR spectroscopy revealed that there
was no drug to polymer interactions. The preliminary mucoadhesive
strength studies performed for various polymers using rotating
cylindrical method showed that HPMC had greater mucoadhesive
properties than carbopol and polycarbophil. Microspheres so
prepared were discrete, bulky, free flowing and showed an
average encapsulation efficiency ranging from 50-60%. Particle
size of the microspheres, as determined by the optical microscopy
was found to be between 400-650µm. The prepared formulations
also exhibited a good mucoadhesive strength which was determined
in in vitro conditions through falling film technique
and was compared with ex vivo studies. The microspheres
so prepared also exhibited a good swelling index which confirmed
the strong mucoadhesive property of the formulation. Metoprolol
release from the multiparticulate system was regulated and
extended until 12 hours and exhibited a non fickian drug release
kinetics approaching to zero order, as evident from the release
rate exponent values which varied between 0.57 to 0.73. The
stability studies performed on the optimized batches at 40
°C
/ 75% RH for 90 days indicated no significant change in the
physicochemical properties.
[Back to top]
Recent Advances in Pelletization Technique for Oral
Drug Delivery: A Review
Md. Akhlaquer Rahman, Alka Ahuja, S. Baboota,
Bhavna, Vikas Bali, Nitin Saigal and Javed Ali
[Full
Text Article]
Multiparticulate dosage forms are receiving a great deal
of attention as alternative system for oral drug delivery.
The present review outlines the recent findings on the manufacturing
and evaluation of spherical pellets published over the past
decade. The techniques namely extrusion-spheronization, hot
melt extrusion, freeze pelletization, cryopelletization have
been discussed along with parameters affecting pelletization.
Evaluation of quality of the pellets is discussed with reference
to the size distribution, shape, surface morphology, specific
surface area, friability, tensile strength, density, porosity,
disintegration time and in vitro dissolution studies
of pellets. The use of multiparticulate dosage forms as a
promising system for the oral delivery of many therapeutic
agents has also been examined in the current review.
[Back to top]
Development and Evaluation of Elementary Osmotic Pump
of Highly Water Soluble Drug: Tramadol Hydrochloride
Pramod Kumar, Sanjay Singh and
Brahmeshwar Mishra
[Full
Text Article]
In the present study Elementary osmotic pump (EOP) of
highly water soluble drug tramadol hydrochloride (TRH) was
developed and evaluated. Target release profile was selected
and different variables were optimized to achieve the same.
Formulation variables like levels of swellable polymer (10-21.87
%) and plasticizer (0-20% w/w of polymer), and coat thickness
of semipermeable membrane (SPM) were found to affect the drug
release from the developed formulations. TRH release was directly
proportional to the level of plasticizer and osmotic pressure
generated by osmotic agent but inversely proportional to the
level of swellable polymer within the core and coat thickness
of SPM. Drug release from developed formulations was independent
of pH and agitation intensities of release media. Burst strength
of the exhausted shells increased with increase in coat thickness
but decreased with increase in level of plasticizer. The in-vitro
results of the developed formulations were compared
with performance of standard marketed formulation of TRH.
The developed formulation provided more prolonged and controlled
TRH release as compared to marketed formulation. The manufacturing
procedure was found to be stable during six months of accelerated
stability study.
[Back to top]
Development and Characterization of Mucoadhesive Buccal
Patches of Salbutamol Sulphate
Rajesh Singh Patel and S.S. Poddar
[Full
Text Article]
Mucoadhesive patch releasing the drug in the oral cavity
at predetermined rate may present distinct advantages over
traditional dosage forms such as tablets, gels and solutions.
The present study was concerned with the preparation and evaluation
of mucoadhesive buccal patches for the controlled systemic
delivery of Salbutamol sulphate to avoid first pass hepatic
metabolism. The developed patches were evaluated for the physicochemical,
mechanical and drug release characteristics. The patches showed
desired mechanical and physicochemical properties to withstand
environment of oral cavity. The in-vitro release
study showed that patches could deliver drug to the oral mucosa
for a period of 7 h. the patches exhibited adequate stability
when tested under accelerated conditions.
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