Recent Patents on Drug Delivery & Formulation (v.7, #2)

Recent Advances in Pulsatile Oral Drug Delivery Systems by Stavros N. Politis, Dimitrios M. Rekkas (87-98).
It is well established that several diseases exhibit circadian behavior, following the relevant rhythm of thephysiological functions of the human body. Their study falls in the fields of chronobiology and chronotherapeutics, thelatter being essentially the effort of timely matching the treatment with the disease expression, in order to maximize thetherapeutic benefits and minimize side effects. Pulsatile drug delivery is one of the pillars of chronopharmaceutics,achieved through dosage form design that allows programmable release of active pharmaceutical ingredients (APIs) tofollow the disease's time profile. Its major characteristic is the presence of lag phases, followed by drug release in a varietyof rates, immediate, repeated or controlled. The scope of this review is to summarize the recent literature on pulsatileoral drug delivery systems and provide an overview of the ready to use solutions and early stage technologies, focusing onthe awarded and pending patents in this technical field during the last few years.

Cationic Liposomes as Non-viral Vector for RNA Delivery in Cancer Immunotherapy by Micaela T. Vitor, Patricia C. Bergami- Santos, Jose A.M. Barbuto, Lucimara G. de la Torre (99-110).
This review presents the current status in the use of liposomes as non-viral vector for nucleic acid delivery incancer immunotherapy. Currently, cancer treatment uses surgery, radiotherapy and/or chemotherapy. The search for newstrategies to improve the efficiency of conventional treatments is a challenge, and biological therapy has emerged as apromising technique. Immunotherapy is a branch of biological therapy that uses the body's immune system to detect anddestroy cancer cells. One immunotherapy approach is the activation of T lymphocytes from cancer patients by dendriticcells (DCs) loaded with tumor antigens. Among different antigens, mRNA coding the tumor antigens is advantageous dueto its capability to be amplified from small amounts of tumor tissue, its safety because it is easily degraded without integratinginto the host genome, and it does not need to cross the nuclear barrier to exert its biological activity. Nanotechnologyis an approach to deliver tumor antigens into DCs. Specially; we review the use of nanoliposomes in the field of cancertherapy because cationic liposomes can be used as non-viral vectors for mRNA delivery. Aside from the promise ofliposomes, the development of scalable processes and facilities to the use this individualized therapy is still a challenge.Thus, we also present the recent techniques used for liposome production. In this context, the integration between technologicalknowledge in the production of cationic liposomes and immunotherapy using mRNA may contribute to the developmentof new strategies for cancer therapy.

Oral bioavailability is the major problem when a poorly water-soluble active agent is delivered via oral route.To overcome such problems, solid dispersion systems have been demonstrated in literature to enhance the dissolutionproperty of poorly water-soluble drugs. In the present review, the important aspects to be considered during preparation ofsolid dispersion systems viz., properties of polymer and preparation techniques of solid dispersion which affect thedissolution rate are discussed. Formulation and evaluation techniques for solid dispersions have been described. Thefinal section of article highlights the recent patents and studies related to solid dispersion systems.

Solubilization of Poorly Water-Soluble Drugs Using Solid Dispersions by Thao T.-D. Tran, Phuong H-L. Tran, Tran N. Khanh, Toi V. Van, Beom-Jin Lee (122-133).
Many new drugs have been discovered in pharmaceutical industry and exposed their surprised potentialtherapeutic effects. Unfortunately, these drugs possess low absorption and bioavailability since their solubility limitationin water. Solid dispersion (SD) is the current technique gaining so many attractions from scientists due to its effect on improvingsolubility and dissolution rate of poorly water-soluble drugs. A number of patents including the most recent inventionshave been undertaken in this review to address various respects of this strategy in solubilization of poorly watersolubledrugs including type of carriers, preparation methods and view of technologies used to detect SD properties andmechanisms with the aim to accomplish a SD not only effective on enhanced bioavailability but also overcome difficultiesassociated with stability and production. Future prospects are as well discussed with an only hope that many developmentsand researches in this field will be successfully reached and contributed to commercial use for treatment as much aspossible.

Preparations of pulmonary surfactant are used for the treatment of respiratory distress syndrome in a newborn.Their applicability as a method of routine for lung diseases beyond the neonatal period is questionable. Some publicationsfrom the former Soviet Union (SU) have reported on successful surfactant therapy of ARDS in children and adults as wellas for inhalation injuries, pneumonia, and tuberculosis. Bronchoscopy was used and recommended as a method of surfactantdelivery for ARDS, some types of pneumonia and tuberculosis. Manufacturing processes of surfactant preparationsfrom bovine lung and amniotic fluid, described by Russian patents, and bronchoscopy as a delivery mode are discussedhere. A concluding point is that some reports from the former SU about administration of exogenous surfactant in pulmonaryconditions, excluding those with primary surfactant deficiency, are only partly confirmed by the international literature.

Recent Patents and Advances on Anti - Tuberculosis Drug Delivery and Formulations by Chintan Vora, Riddhish Patadia, Karan Mittal, Rajashree Mashru (138-149).
Tuberculosis has remained, unambiguously, a significant health care problem since long times, particularly indeveloping countries. The endeavoring battle against multi drug resistant TB, multiple dosing, their prominent side effectsand bioavailability hiccups related to fixed dose combinations has undeniably become a Herculean task indicating rigorousresearch requirement in anti TB drug therapy. In view of the fact that patenting a drug molecule, a drug delivery systemor a formulation has been very fruitful for the growth and sustainment of pharmaceutical industry, a meticulous reviewof recent developments, providing a balanced view on merits/demerits, will facilitate researchers to update themselves,thereby focusing their research in more relevant areas to furnish desired quality traits. This article reviews the presentscenario in terms of drug delivery approaches for TB chemotherapy. The review encompasses and summarizes recentpatents and advances on variegated facets of dosage forms, together with from conventional solid oral to novel controlledrelease oral formulations and additionally alternative weapons for anti TB drug delivery. A critical review of multidisciplinaryapproaches to boost anti TB therapy may facilitate the scientists to resolve existing technological gaps.

Osmotic Drug Delivery Systems: Basics and Design Approaches by Chinam N. Patra, Suryakanta Swain, Jammula Sruti, Allupati P. Patro, Kahnu C. Panigrahi, Sarwar Beg, Muddana E.B. Rao (150-161).
Osmotic drug delivery system utilizes the principles of osmotic pressure for the controlled delivery of activepharmaceutical ingredient at a predetermined zero order rate. An appropriately designed osmotic drug delivery is notinfluenced by different physiologic factors but affected by pharmaceutical factors, which play a pivotal role in modulatingthe release of drug. The present review critically discussed about the factors affecting drug release from the delivery systemsuch as solubility, osmotic pressure, size of delivery orifice and membrane characteristics. The major arena of thisreview is to highlight about the different types of osmotic drug delivery systems such as implantable, single chamber,multi chamber osmotic pumps and several specialized type of osmotic pumps. Apart from that this system is a versatiletechnology useful for delivery of drugs with varying solubility. The additional properties of this delivery system can alsoexhibit pulsatile release, burst release and colon targeting of drug. Because of its versatility, this above system seems tohave promising approach which can result in improved safety profile, stable drug concentrations, uniform drug effects anddosing frequency. Current review also briefly discussed about the patents related to delivery of drugs by the principleosmotic pressure.

Patent Selections: (162-164).