Showing papers in "Recent Patents on Drug Delivery & Formulation in 2011"

Parenteral drug delivery: a review.

Abstract: The parenteral route of administration is the most effective route for the delivery of the active pharmaceutical substances with narrow therapeutic index, poor bioavailability especially for those drugs, prescribed to unconscious patients. To maintain a therapeutic effective concentration of the drug, it requires frequent injections which ultimately lead to patient discomfort. In parenteral drug delivery, major progress has been done in the field of formulation technologies so as to provide a targeted and sustained release of drug in predictable manner. The present article reviews recent patents and major advancements in parenteral drug delivery systems along with general introduction. This article also deals with importance of novel systems in drug delivery to overcome the problems associated with conventional parenteral drug delivery systems.

SLN, NLC, LDC: state of the art in drug and active delivery.

Abstract: Drug delivery system focuses on the regulation of the in vivo dynamics, in order to improve the effectiveness and safety of the incorporated drugs by use of novel drug formulation technologies. Lipids such as fatty acids, triglycerides, vegetable oils and their derivatives, used for developing multiparticulate dosage forms, may be available in solid, semi-solid or liquid state. Solid lipid nanoparticles (SLNs), nanostructured lipid carriers (NLCs) and lipid drug conjugate (LDCs) nanoparticles are novel lipid drug delivery systems. They were devised to address some of the challenges of conventional drug delivery systems ranging from low drug encapsulation efficiency to low bioavailability of Biopharmaceutical Classification Systems (BCS) class II and class IV drugs. SLNs are based on melt-emulsified lipids, which are solid at room temperature and consist of physiologically well tolerated ingredients often generally recognised as safe. NLCs are colloidal carriers characterized by a solid lipid core consisting of a mixture of solid and liquid lipids, and having a mean particle size in the nanometer range. LDC are nanoparticles contain drugs linked to lipid particles. This minireview highlights these three different but related technologies in lipid drug delivery. The objectives of their introduction, current applications, major challenges and some patented formulations are highlighted.

Microneedles and their applications.

Abstract: Microneedle mediated microporation has proved its potential to enhance the delivery of therapeutic drug molecules through skin over the last one decade. Several patents have been granted and cutting edge research is going on particularly for the delivery of biopharmaceuticals (macromolecules like protein or peptides). The technology involves use of micron sized needles made of diverse materials to form microchannels into the stratum corneum (or deeper), outermost barrier layer of the skin. These microchannels are deep enough to facilitate efficient drug delivery through disrupted stratum corneum but short enough to avoid bleeding or pain. So far, the microneedle technology has been explored for drug and vaccine delivery through transcutaneous route. However, the miniaturized nature of these microneedles and anticipated minimal invasiveness has led the scientists to explore and patent its possible use for several other applications.The use of this technology in combination with other enhancement techniques has also gained recent attention. This review article focuses on the latest developments in the field of microneedles as described in patent and research literature. Comprehensive review of several topics including device design/fabrication, formulation development, safety/regulatory issues, therapeutic applications and major challenges in the commercialization of microneedles as medical devices has been presented here.

Review of patents on microneedle applicators.

Abstract: Transdermal drug delivery offers certain advantages over conventional oral or parenteral administration. However, transdermal delivery is not available to many promising therapeutic agents, especially high molecular weight hydrophilic compounds. This is due to the excellent barrier property of the superficial skin layer, the stratum corneum (SC). Only drugs with very specific physicochemical properties (molecular weight < 500 Da, adequate lipophilicity, and low melting point) can be successfully administered transdermally. Of the several active approaches used to enhance the transport of drugs through the SC, the use of microneedles (MNs) has recently been shown to be very promising and has attracted considerable attention by researchers from both industry and academia. MNs, when used to puncture skin, will by-pass the SC and create transient aqueous transport pathways of micron dimensions and enhance the transdermal permeability. However, for effective performance of these MNs in drug delivery applications, irrespective of the type, material, height and density, it is imperative that they penetrate into the skin with the greatest possible accuracy and reproducibility. Due to the inherent elasticity and irregular surface topography of the skin, it remains a major challenge to the reproducibility of MN penetration. Therefore, in order to achieve uniform and reproducible MN penetration into skin, an external source of assistance could be very useful. Accordingly, this review deals with various innovative applicator designs developed by industry and research centres in the context of effective application of MN arrays for transdermal drug delivery, as disclosed in the recent patent literature.

Self-Assembling Peptides: Implications for Patenting in Drug Delivery and Tissue Engineering

Abstract: In this paper, a comprehensive review of recent patents concerning the molecular self-assembly of peptides, peptide amphiphiles and peptidomimetics into molecules through nanoarchitectures to hydrogels is provided. Their potential applications in the field of drug delivery and tissue engineering have been highlighted. The design rules of this rapidly growing field are centered mainly on the construction of peptides in the form of peptide amphiphiles, aromatic short peptide derivatives, all-amino acid peptide amphiphiles, lipidated peptides with single and multiple alkyl chains and peptide-based block copolymers and polymer peptide conjugates. The interest in patenting of self-assembling peptides is also driven by their type (I, II, III and IV) and their ability to form well-regulated highly-ordered structures such as β- sheets/β-hairpins, α-helices/coiled coils and to hierarchically self-organize into supra-molecular structures. The applicability of these systems in cell culture scaffolds for tissue engineering, drug and gene delivery and as templates for nanofabrication and biomineralization has inspired various groups over the globe. This resulted in development of selfassembling peptides as synthetic replacements of biological tissues, designing materials for specific medical applications, and materials for new applications such as diagnostic technologies. Furthermore, biologically derived and commercially available systems are also discussed herein along with a brief account of various awarded and pending patents in the past 10 years. An overview of the diversity of the patent applications is also provided for self-assembling systems based on nano- and/or micro-scale such as fibers, fibrils, gels, hydrogels, vesicles, particles, micelles, bilayers and scaffolds.

Therapeutic applications of nanoemulsion based drug delivery systems: a review of patents in last two decades.

Abstract: Nanoemulsions have garnered considerable attention in research as well as in therapeutics due to their advantages like thermodynamic stability, optical clarity, ease of preparation, and unique property of behaving as supersolvent for solubilizing both hydrophobic and hydrophilic solutes. Due to above mentioned attributes, nanoemulsions find numerous applications in diagnosis as well as therapy of diseases. Hence, the aim of the current review is to recapitulate these applications of this novel drug delivery system by discussing the patents governing various applications of this system.

New methods for lipid nanoparticles preparation.

Abstract: Lipid nanoparticles have attracted many researchers during recent years due to the excellent tolerability and advantages compared to liposomes and polymeric nanoparticles. High pressure homogenization is the main technique used to prepare solid lipid nanoparticles (SLN) encapsulating different type of drugs, however this method involves some critical process parameters. For this reason and in order to overcome patented methods, different production techniques for lipid nanoparticles have been widely investigated in recent years (last decade). The paper reviews new methods for lipid nanoparticles preparation, and their recent applications in pharmaceutical field, especially focusing on coacervation, microemulsions templates, supercritical fluid technology, phase-inversion temperature (PIT) techniques. References of the most relevant literature and patents published by various research groups on these fields are provided.

Recent advances in intraocular drug delivery systems.

Abstract: Vitreoretinal diseases are refractory to both topical and systemic pharmacological approaches because of specific environment of the eye. That is, the cornea, the sclera, nasolacrimal drainage of tears, frontward stream of aqueous humor, blood-aqueous barrier, and blood-retinal barrier strictly limit penetration and diffusion of drug into the retina. However, recent advances in intraocular drug delivery systems (DDS) have enabled drug to be delivered effectively into the eye. Clinically successful or promising cases involve non-biodegradable implants and inserts, biodegradable inserts and microparticles, intravitreal or sub-Tenon's injection of triamcinolone acetonide, and a photodynamic therapy (PDT) with verteporfin, a photosensitizer. More recently, a variety of pharmacological challenges to treat exudative age-related macular degeneration and macular edema are proceeding into clinical trials, as soon as antivascular endothelial growth factor (anti-VEGF) therapies have been proved to be effective by repeated intravitreal injections. In the near future, DDS must be required not only to develop a new treatment modality but also to improve efficacy and/or reduce injection numbers of currently available drugs. Here we introduce controlled release of drug and discussion of recent patents with biodegradable or non-biodegradable implants and drug targeting by modification of systemically administered drug

Exploring novel approaches to vaginal drug delivery.

Abstract: Vaginal route serves as a potential site of drug administration for local and systemic absorption of a variety of therapeutic agents. Despite being a non- invasive route of drug administration, the vagina has not been extensively explored as compared to other routes. Intravaginal drug delivery has been traditionally restricted to delivery of antinfectives to the local vaginal cavity. Concerted efforts have been made in the recent past to rediscover the vaginal route as a potential route for the delivery of therapeutically important molecules, proteins, peptides, small interfering RNAs, oligonucleotides, antigens, vaccines and hormones. The understanding of vaginal physiology has led to the design of specific intravaginal drug delivery systems to reach the systemic circulation. To overcome the limitations of conventional dosage forms administered through vaginal route various novel approaches like the use of mucoadhesive or bioadhesive polymers, pH- or temperature-sensitive polymers, liposomes, nanoemulsions, nanoparticles, vaginal inserts, multiple emulsions and hydrogels have been designed which enable controlled and prolonged release of drugs. The present article is a comprehensive review of the research and patents encompassing conventional dosage forms used for vaginal drug delivery with emphasis on newer platform technologies pertaining to intravaginal administration.

Lipid nanoparticles as vehicles for macromolecules: nucleic acids and peptides.

Abstract: Traditional drug delivery systems are not efficient for peptide, protein and nucleic acid (plasmid DNA, oligonucleotides or short interfering RNA) delivery, thereby LNP have been exploited as potential delivery and targeting systems of these molecules. Since their discovery in the early 90's several research groups have focused their efforts on the improvement of this kind of nanocarriers in terms of effectiveness and safety. This review features the recent and most relevant patents related to these topics, with particular attention to targeting and protection from environmental agents. Moreover, in the case of nucleic acids strategies to improve transfection mediated by lipid nanoparticles (entrance to the cells, intracellular distribution or going through nuclear envelope) will be assessed. Regarding peptides and proteins, enhancement of encapsulation efficiency and absorption through mucoses are the main studied drawbacks. Finally, this work also includes a summary of the existing patents about the use of LNP as immune response adjuvants by using either plasmid DNA or proteins.

Pelletization processes for pharmaceutical applications: a patent review.

Abstract: Pellets exhibit major therapeutic and technical advantages which have established them as an exceptionally useful dosage form. A plethora of processes and materials is available for the production of pellets, which practically allows inexhaustible configurations contributing to the flexibility and versatility of pellets as drug delivery systems. The scope of this review is to summarize the recent literature on pelletization processes for pharmaceutical applications, focusing on the awarded and pending patents in this technical field. The first part of the article provides an overview of innovation in pelletization processes, while the second part evaluates their novel applications.

Recent Advances and Patents in Solid Dispersion Technology

Abstract: High lipophilicity and high lattice energy of drugs, which result in poor solubility are major real challenges in the pharmaceutical industry for the successful development and commercialization of suitable dosage forms. Therefore various formulation strategies like complexation, lipid based systems, micronization, nanonization, co-crystals, solid dispersions, solubilization etc. have been investigated to resolve the problems associated with solubility related oral bioavailability of poorly water soluble drugs. This article focuses on solid dispersions which is used as one of the formulation strategies to improve the solubility and bioavailability of BCS class II drugs. The present review discusses the fundamentals of solid dispersions, their formulation techniques including various carriers used, their applications, limitations as well as provide an insight into the various alternative approaches to overcome problems associated with solid dispersions. This review also discusses some important aspects of solid dispersion like phase transition, importance of Tg for solid dispersion, controlled release formulations, IVIVC, and the prospect of innovative solid dispersions. Furthermore, the different patents highlighting the applications of solid dispersions have also been comprehensively discussed in the present review.

Intelligent Hydrogels for Drug Delivery System

Abstract: Intelligent hydrogel, also known as smart hydrogels, are materials with great potential for development in drug delivery system. Intelligent hydrogel also has the ability to perceive as a signal structure change and stimulation. The review introduces the temperature-, pH-, electric signal-, biochemical molecule-, light- and pressure- sensitive hydrogels. Finally, we described the application of intelligent hydrogel in drug delivery system and the recent patents involved for hydrogel in drug delivery.

Recent patents on oral combination drug delivery and formulations.

Abstract: Oral combination drug delivery systems have been proven to be highly beneficial and vital in the treatment of several dreadful diseases such as cancer, HIV (AIDS) and tuberculosis. Further, pharmaceutical companies have often explored the strategy of combination drug therapy for treating diseases such as diabetes (Type 2), cardiovascular diseases, central nervous system (CNS) disorders, and for treating several other microbial infections. Patenting combination drug delivery systems and formulations has been proven to be very beneficial for the sustainment and growth of pharmaceutical industry. Several pharmaceutical companies have explored this opportunity in extending the life cycle of their blockbuster molecules, and providing additional sources of revenues when the new chemical entity (NCE) discovery is scarce. The article reviews some recent combination formulation patents and patent publications, particularly the US patents and patent applications, relevant to oral delivery of pharmaceuticals. Examples of some oral combination products on the US and worldwide market are presented. Patents and patent applications on combination oral formulations relevant to analgesics (including anti-inflammatory and antipyretics), cardiovascular system (CVS) products, antibacterial and antiviral, and central nervous system (CNS) products are briefly discussed.

Powdered Lipid Nano and Microparticles: Production and Applications

Abstract: This review details articles and recent patents in an emerging topic called powdered form of nano- and microparticles. Solid lipid particles were developed in the early 1990s and since, they have been considered as promising drug delivery systems, especially in providing a sustained release profile of the encapsulated drug. This kind of drug delivery system has several advantages, due to its physiological composition. It is generally well tolerated by the human body and are relatively stable during storage in comparison with other carriers like liposomes. The description of these powdered lipid particles, their different production processes and their applications are the focus of the article.

An updated patent review on ocular drug delivery systems with potential for commercial viability.

Abstract: The eye due to its special attributes is an effortlessly accessible location for topical drug administration. Topical administration not only provides local targeting of drugs but also offers a better control over the systemic delivery. Bioavailability of drugs from ocular dosage forms is dependent to the precorneal loss factors (physiological and anatomical constraints of eye) thus, very small fraction of the drug is absorbed through ocular route. The effective dose of medication administered ophthalmically may be altered by changing the formulation. Various research reports have been documented for ocular drug delivery, both on academic level as well as commercial level resulting in augmented increase in the numbers of patents in this field. The primary objective of the present review is to provide an overview of the ocular drug delivery systems with special emphasis on the intellectual aspects of these systems. This paper also attempts to extend the information on ocular drug delivery systems already existing in the literature by focusing on the update on the patents granted as well as applications published for these systems during the last decade.

Oral fast-release solid dispersion-paradigm shift to nanoparticles

Abstract: Design of oral fast-release solid dispersion of poorly water-soluble drugs has been a great challenge over past decades on issues of drug recrystallization, drug polymorphism, formulation limited to low drug-to-carrier ratio and drug particle aggregation in matrix. The complexity in solid dispersion design is envisaged to be resolvable by the use of nanoparticulate system as solid dosage form. This manuscript reviews several patented processing approaches of nanoparticulate solid dispersion that have been reported recently. Through drug nanoencapsulation, a higher content of drug may be delivered with less aggregation via placing the same drug mass in a greater number of tinier carriers. Nanoencapsulation, by its own process of formation, brings about submicron particles. Keeping drug in these nanoparticles, a remarkable rise in specific surface area of drug is realized for dissolution. The augmentation of drug dissolution can be sufficiently high to the extent that the influences of polymorphism and crystallization phenomenon on drug dissolution in a solid dispersion may be negligible.