Recent Patents on Drug Delivery & Formulation - Volume 12, Issue 4, 2018

Background: Nanotechnology-based drug delivery approach has emerged as a promising field, where different kinds of formulations are developed for therapeutic applications. Inflowing of nanomedicine developed through various biomaterials appears to be a game changer in the domain of pharmaceutical and biotechnological industries. Nanomedicines propose to overcome the major constraints of conventional medicine of low solubility and stability, non-adequate pharmacokinetic profiles and side effects. Objectives: Mesoporous Silica Nanoparticles (MSNs) have garnered significant attention in biomedical applications for its multifunctionality. The porous structure of MSNs provides the opportunity for heavy drug loading, controlled release and ligand functionality. From last decades, a lot of interest has been generated owing to the better drug delivery attributes of MSNs to introduce unique biological effects for its suitable therapeutic application. Methods: The review article gives an insight into the current advancement of usage of MSNs in drug delivery for cancer, non-cancer and biosensors based biomedical applications along with technology that is protected by patents. Conclusion: The future success of MSNs is widened because of their valuable characteristic that easily combines with various functionalities which would display enormous potential translational possibilities.

Skeletal muscle is a highly-specialized tissue that is capable of contractile function and able to withstand and adapt to daily mechanical and physiological stress. Musculoskeletal disorders, including muscular dystrophies, result in chronic pain and disability, reduced quality of life, burden on family, and increased healthcare costs. Although several mechanisms have been identified for muscle injury and regeneration, mechanisms of these diseases are poorly understood, and targeted and effective pharmacologic treatment(s) are not available. More research is needed in this area in order to develop effective treatment regimens. The purpose of this review is to discuss known mechanisms of muscle injury and repair, and highlight some recent patents and research developments for treatment of skeletal muscle disorders.

Background: For the past few decades, there has been considerable research interest in drug delivery strategies using nanoparticulate systems as carriers for a wide range of active pharmaceutical ingredients. Objective: It is known that nanoparticulate drug delivery systems comprise a wide variety of dosage forms including nanospheres, micelles, solid lipid nanoparticles, nanoliposomes, dendrimers, magnetic nanoparticles, and nanocapsules. Methods: This review describes nanocapsule preparation techniques and their applications for the treatment of several diseases using patents and examples from the literature. Results: Nanocapsules are vesicular systems consisting of an inner liquid core (aqueous/oily) surrounded by a polymeric wall that has immense potential as drug carriers because of the many advantages like improving poor aqueous solubility, stabilizing drugs by protecting the molecule from the environment, providing the desired pharmacokinetic profile, allowing controlled release, as well as facilitating oral administration. Conclusion: The present study discusses and summarizes patents related to preparation methods of and recent studies from the last 10 years on nanocapsules as drug delivery systems.

Aim and Background: The rationale of this study is that, treatment of asthmatic Guinea pig with combined administration of Montelukast sodium and Green Tea Extract (GTE) as a single capsule will mitigate the inflammatory injury in the airways and weaken the asthmatic response. Recent patents for the treatment of asthma researched a polyphenolic alternatives for antiasthmatic combination therapy, especially for those patients who remains unresponsive or poorly responsive for current asthma therapy (US7232585B2). Synergistic activity of green tea polyphenols and therapeutic, prophylatic agents are also reported in some recent patents (US20120172423A1, US20150320696A1). The present work is therefore aimed, to study the effect of Montelukast Sodium capsules coformulated with GTE on oxidative stress markers including Malondialdehyde (MDA), Glutathione (GSH) in different organs and Oxygen Radical Absorbance Capacity (ORAC) assay in plasma. Materials and Methods: Guinea pigs were placed in histamine chamber and exposed to an aerosol challenge of 0.2% w/v histamine dihydrochloride in distilled water using pressurized air driven nebulizer at a pressure of 0.05 MPa-0.106 MPa for one week. After that, they were divided in to four groups of three each; control, asthmatic control, asthmatic treated with marketed preparation and asthmatic received developed capsules. After oral administration of formulations for three days, pigs were scarificed and oxidative stress markers level including cytoarchitectural manifestation in tissues was studied. Results: In comparison with the healthy control group, MDA level of the asthmatic animal liver and lung was found to be elevated as 0.059 ± 0.031(p < 0.002) and 0.802 ± 0.310 (p < 0.005) respectively, whereas GSH level was declined as 13.223 ± 1.485 (p < 0.0001) in liver and 3.037 ± 0.282 (p < 0.0004) in lung tissues. TAC of asthmatic animal plasma was low as 2.132 ± 0.986 mM Trolox Eq/L (p < 0.009). The level of these biomarkers reverts back towards normal after treatment with marketed and developed formulation, although treatment with developed formulation was more efficacious since it was coformulated with GTE, which acts as an adjuvant for the management of inflammatory disease like asthma. Conclusion: It is contemplated that, use of GTE as an adjuvant to anti leukotriene drug played a significant role in asthma management by reducing oxidant injury. Since, studies in animals do not directly translate to human biology, further multi-control studies with better sampled patient population and more number of patients are needed.

Background: During the recent two decades, the development of mucoadhesive drug delivery system has been gained tremendous importance to cure many recurrent diseases of the oral cavity. The drug delivery through the buccal route is quite challenging due to limited absorption area, movements of the target region and regular flow of saliva lead to the sub-therapeutic drug level in the buccal region. Objective: The aim is to develop unidirectional release mucoadhesive buccal film for the mucosal delivery of Benzydamine Hydrochloride (WO2016126217Al, EP0812193B1) and evaluate the effects of a different grade of HPMC polymer (US5980942A) with the presumption to prolong the residence time and therapeutic effectiveness at the target site. Methods: Mucoadhesive buccal films were prepared by solvent casting evaporation method by employing different grades of HPMC as mucoadhesive and rate controlling polymer. Total twenty-four formulations were developed using ethyl cellulose as a backing layer. The prepared films were subjected to various physicochemical parameters. Results: The physicochemical parameters were found to be varied according to the type and concentration of polymer used. On the basis of in vitro drug release, desired ex-vivo mucoadhesive time, mucoadhesive force the formulations F4, F9, F14 and F19 were subjected to ex vivo drug permeation study. The F14 film containing 1% w/v of HPMC K50M was considered optimized final formulation due to higher ex vivo drug permeation. Drug-excipient compatibility was confirmed by FTIR and DSC. XRD of final formulation revealed the amorphous nature of drug. SEM indicated the perfect binding between backing and adhesive layer. Conclusion: The developed mucoadhesive buccal film having adequate physicochemical properties was capable to provide prolonged residence time and sustained delivery as compared to existing conventional therapies.