| Recent
Patents on Drug Delivery & Formulation
ISSN: 1872-2113
Recent Patents on Drug Delivery
& Formulation
Volume 1, Number 1, February
2007
Contents
Nanocarriers for Systemic and Mucosal Vaccine
Delivery Pp. 1-9
Aliasgar Shahiwala, Tushar K. Vyas and Mansoor M. Amiji
[Abstract] [Full
Text Article]
Development of Dry Powder Inhalers Pp. 11-21
Mahavir B. Chougule, Bijay K. Padhi, Kaustubh A. Jinturkar
and Ambikanandan Misra
[Abstract] [Full
Text Article]
Innovations in Transdermal Drug Delivery: Formulations
and Techniques Pp. 23-36
Ashok K. Tiwary, Bharti Sapra and Subheet Jain
[Abstract] [Full
Text Article]
Engineered Nanoparticles in Cancer Therapy
Pp. 37-51
Natalie P. Praetorius and Tarun K. Mandal
[Abstract] [Full
Text Article]
Modified-Release Solid Formulations for Colonic Delivery
Pp. 53-63
Brahma N. Singh
[Abstract] [Full
Text Article]
Smart Polymer Based Delivery Systems for Peptides
and Proteins Pp. 65-71
Khaled Al-Tahami and Jagdish Singh
[Abstract] [Full
Text Article]
Time-Controlled Pulsatile Delivery Systems for Bioactive
Compounds Pp. 73-79
Anil K. Anal
[Abstract] [Full
Text Article]
Cell Encapsulation in Mammal Reproduction
Pp. 81-85
Maria L. Torre, Massimo Faustini, Klinger M. E. Attilio
and Daniele Vigo
[Abstract] [Full
Text Article]
Patent
Annotations Pp. 87-91
Patent
Selections Pp. 93-103
Abstracts
[Back to top]
Nanocarriers for Systemic and Mucosal Vaccine Delivery
Aliasgar Shahiwala, Tushar K. Vyas and Mansoor M. Amiji
[Full
Text Article]
Over the past several years, immunization and treatment of
infectious diseases has undergone a paradigm shift. Stemming
from the vaccine research and development, not only a large
number of disease-specific vaccines have been developed, but
also enormous efforts have been made to improve the effectiveness
of vaccines in order to provide optimal immunization. Introduction
of nanotechnology and the development of nanocarrier-based
vaccines have started to receive a lot of attention in order
to provide effective immunization through better targeting
and by triggering antibody response at the cellular level.
Also, in the past several years, attention is placed on routes
of vaccine administration in order to induce both mucosal
and systemic immunity against the pathogen. Through judicious
selection of the nanocarrier systems and the vaccine antigen,
an optimal immunization and protection can be induced. This
review article focuses on the patented applications of nanocarrier-based
vaccine formulations and delivery. We have examined the United
States patent literature to select inventions that specifically
address this strategic approach for prevention of infectious
diseases.
[Back to top]
Development of Dry Powder Inhalers
Mahavir B. Chougule, Bijay K. Padhi, Kaustubh A. Jinturkar
and Ambikanandan Misra
[Full
Text Article]
Development of dry powder inhalers involves powder recrystallization,
formulation, dispersion, delivery, and deposition of the therapeutic
agent in different regions of the airways in prophylaxis/
treatment/ diagnosis of pulmonary and systemic disorders.
Conventional powder production by crystallization and milling
has many limitations resulting into development of alternative
techniques to overcome the problems. In the last decade many
patents have been filed claiming improvement in aerosol performance
of dry powder inhalers through the use of (i) incorporation
of fines of carrier particles to occupy active sites on the
surface and use of hydrophobic carriers to facilitate deaggregation
through reduced surface energy and particle interaction (ii)
reducing aerodynamic diameters through particle engineering
and incorporating drug into porous or low particle density,
and/or (iii) preparing less cohesive and adhesive particles
through corrugated surfaces, low bulk density, reduced surface
energy and particle interaction and hydrophobic additives.
Moisture within dry powder inhaler (DPI) products has also
been shown to influence aerosol performance via capillary
force and electrostatic interaction. Better understanding
of particle forces and surface energy has been achieved by
the use of sophisticated analytical techniques. Understanding
the intricacies of particle shape and surface properties influencing
specific lung deposition has been further facilitated by the
availability of newer and advanced softwares. A critical review
of recent patents claiming different approaches to improve
lung deposition of dry powder inhalers will help in deciding
the focus of the research in the area of technological gaps.
[Back to top]
Innovations in Transdermal Drug Delivery: Formulations
and Techniques
Ashok K. Tiwary, Bharti Sapra and Subheet Jain
[Full
Text Article]
The transdermal route of drug delivery has attracted researchers
due to many biomedical advantages associated with it. However,
excellent impervious nature of skin is the greatest challenge
that has to be overcome for successfully delivering drug molecules
to the systemic circulation by this route. Various formulation
approaches used to systemically deliver drug molecules include
use of prodrugs/lipophilic analogs, permeation enhancers,
sub saturated systems and entrapment into vesicular systems.
Further, the adhesive mixture, physical system of the delivery
system and release liner influence drug release and its permeation
across the skin. In addition, great strides in designing delivery
systems for maximizing percutaneous drug permeation without
comprising with ease of therapy cannot be neglected in improving
functionality of transdermal drug delivery systems. This article
deals with the innovations pertaining to formulation and techniques
as described in recent patents.
[Back to top]
Engineered Nanoparticles in Cancer Therapy
Natalie P. Praetorius and Tarun K. Mandal
[Full
Text Article]
Intense research has led to a more comprehensive understanding
of cancer at the genetic, molecular, and cellular levels providing
an avenue for methods of increasing antitumor efficacy of
drugs while reducing systemic side effects. Nanoparticulate
technology is of particular use in developing a new generation
of more effective cancer therapies capable of overcoming the
many biological, biophysical, and biomedical barriers that
the body stages against a standard intervention. Nanoparticles
show much promise in cancer therapy by selectively gaining
access to tumor due to their small size and modifiability.
Typically, though not exclusively, nanoparticles are defined
as submicroscopic particles between 1 and 100 nm. Nanoparticles
are formulated out of a variety of substances and engineered
to carry an array of substances in a controlled and targeted
manner. Nanoparticles are prepared to take advantage of fundamental
cancer morphology and modes of development such as rapid proliferation
of cells, antigen expression, and leaky tumor vasculature.
In cancer treatment and detection nanoparticles serve many
targeted functions in chemotherapy, radiotherapy, immunotherapy,
immunodetection, thermotherapy, imaging, photodynamic therapy,
and anti-angiogenesis. Not only are modifying agents allowing
for greater and more accurate tumor targeting, they are also
aiding in the crossing of biophysical barriers such as the
blood brain barrier there by reducing peripheral effects and
increasing the relative amount of drug reaching in the brain.
Moreover, multifunctional nanoparticles perform many of these
tasks simultaneously such as targeted delivery of a potent
anticancer drug at the same time as an imaging material to
visualize the effectiveness of the drug utilized for treatment
follow-up. In this review, several recent US and World patents
developing and modifying nanoparticles for the detection,
analysis, and treatment of cancer are discussed.
[Back to top]
Modified-Release Solid Formulations for Colonic Delivery
Brahma N. Singh
[Full
Text Article]
Solid formulations intended for targeted drug release into
the lower gastrointestinal (GI) tract are beneficial for the
localized treatment of several diseases and conditions, mainly
inflammatory bowel diseases, irritable bowel syndrome and
colon cancer. Also, because of their inherent potential to
delay or avoid systemic drug absorption from the small intestine,
colonic formulations can be utilized for chronotherapy of
diseases which are affected by circadian biorhythms (e.g.,
asthma, hypertension and arthritis), and to achieve clinically
relevant bioavailability of drugs that are poorly absorbed
from the upper parts of the GI tract because of their polar
nature and/or susceptibility to chemical and enzymatic degradation
in the small intestine (e.g., proteins and peptides). The
purpose of this review is to summarize the Recent Patent literature
concerning various modified-release (MR) formulation technologies
that are claimed to provide colonic delivery for a wide array
of therapeutic molecules. These technologies either utilize
a single or a combination of two or more physiological characteristics
of the colon, which includes pH, microflora (enterobacteria),
transit time, and luminal pressure. Accordingly, these technologies
may be grouped under four distinct classes: pH-controlled
(or delayed-release) system, time-controlled (or time-dependent)
system, microbially-controlled system, and pressure-controlled
system. Among these, formulations that release drugs in response
to colonic pH, enterobacteria, or both are most common and
promising.
[Back to top]
Smart Polymer Based Delivery Systems for Peptides
and Proteins
Khaled Al-Tahami and Jagdish Singh
[Full
Text Article]
Biodegradable polymeric systems represent promising means
for delivering many bioactive agents, including peptide and
protein drugs. The importance of these systems grew with the
advancement in the understanding of peptide and protein pharmacology
as well as the ability to mass-produce these compounds. Some
polymers undergo sol-gel transition once administered. In
situ gel formation happens in response to one or a combination
of two or more stimuli. These stimuli include UV-irradiation,
pH change, temperature change, and solvent exchange. These
smart polymeric systems have several advantages over conventional
methods, such as ease of manufacturing, ease of administration,
biodegradability, and the ability to alter release profiles
of the incorporated agents. In the past few years, an increasing
number of in situ gel-forming systems have been investigated
and many patents for their use in various biomedical applications,
including drug delivery, have been reported. In this article,
we introduce the different strategies that have been developed
and patented for the use of smart polymers in delivering peptide
and protein drugs. The advantage, disadvantages, possibilities,
and limitations of each of the smart polymer systems have
been discussed.
[Back to top]
Time-Controlled Pulsatile Delivery Systems for Bioactive
Compounds
Anil K. Anal
[Full
Text Article]
In the body under physiological conditions, many vital functions
are regulated by pulsed or transient release of bioactive
substances at a specific time and site. Thus, to mimic the
function of living systems, it is important to develop new
drug delivery devices to achieve pulsed delivery of a certain
amount of a bioactive compound at predetermined time intervals.
The ability to deliver bioactive compounds and/or therapeutic
agents to a patient in a pulsatile or staggered release profile
has been a major goal in drug delivery research over the last
two decades. The plasma peak is obtained at an optimal time
by timing the drug administration. The number of doses per
day can be reduced. Based on the relevance of potential therapeutic
applications, a variety of design strategies have been formulated
in the pursuit of pulsatile release. Overall, these systems
can be categorized into reservoir, capsular and osmotic devices.
In this review article, several types of dosage forms, including
microparticles, coarse particulates, large solid implants,
hydrogels, osmotic pumps and liposomes, for time-controlled
pulsatile release are discussed. This review describes the
recent patents related to pre-programmed delivery systems,
such as systems with eroding, soluble or rupturable barrier
coatings, and systems with capsular structures.
[Back to top]
Cell Encapsulation in Mammal Reproduction
Maria L. Torre, Massimo Faustini, Klinger M. E. Attilio
and Daniele Vigo
[Full
Text Article]
Cell encapsulation is an evolving branch of biotechnology
with numerous applications including the enhancing of reproductive
performance both in humans and other mammal species. Over
the last twenty years male and female gametes and embryos
have been encapsulated with or without somatic cells, for
different purposes, such as semen controlled release, in
vitro gametogenesis, embryo culture after in vitro
fertilization and cell preservation. In this paper the state-of-the-art
of this field (leaving aside that involving embryonic stem
cells) is reviewed in terms of scientific literature and patent
production. The patents and papers underline a widespread
use of alginate which is a natural anionic, biocompatible,
biodegradable polymer that mimics the extracellular matrix
or the basal membrane and supports cell functions and metabolism.
Gamete and embryo encapsulation techniques tend to fall into
two main groupings: the “classical” three-step
method, and the more recent one-step method. However, all
of these encapsulation techniques are moving towards new,
interesting applications since they can be easily tailor-made
to fit a variety of cell lines.
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