Pharmaceutical Lozenges: Recent Trends and Developments with an Update on Research and Patents

Pharmaceutical oral dosage forms are tremendously preferred by both consumers as well as pharmaceutical manufacturers owing to the plethora of benefits they offer. Lozenges (LZs) are one of the dosage forms that provide a palatable means of drug administration and have great importance with respect to their pharmaceutical applications. LZs offer additional benefits to pediatric and geriatric patients, along with people having associated problems with the gastro-intestinal tract. Dysphagia is a common problem faced by all age groups, which gives rise to the need for LZs. Moreover, the foremost merit presented by the medicated LZs includes its augmented retention time in the oral cavity that results in an enhanced bioavailability for buccal or upper gastro-intestinal disorders. Further, LZs can also be used to bypass the first-pass effect. The present review covers various aspects of LZs such as formulation, manufacturing techniques, evaluation parameters, marketed products, patents, and a compilation of research work that has been done on lozenges as a delivery system.

A comprehensive insight on self emulsifying drug delivery systems

Background: The oral route is a highly recommended route for the delivery of a drug. But most lipophilic drugs are difficult to deliver via this route due to their low aqueous solubility. Selfemulsifying drug delivery systems (SEDDS) have emerged as a potential approach of increasing dissolution of a hydrophobic drug due to spontaneous dispersion in micron or nano sized globules in the GI tract under mild agitation. Objective: The main motive of this review article is to describe the mechanisms, advantages, disadvantages, factors affecting, effects of excipients, possible mechanisms of enhancing bioavailability, and evaluation of self-emulsifying drug delivery systems. Result: Self emulsifying systems incorporate the hydrophobic drug inside the oil globules, and a monolayer is formed by surfactants to provide the low interfacial tension, which leads to improvement in the dissolution rate of hydrophobic drugs. The globule size of self-emulsifying systems depends upon the type and ratio of excipients in which they are used. The ternary phase diagram is constructed to find out the range of concentration of excipients used. This review article also presents recent and updated patents on self-emulsifying drug delivery systems. Self-emulsifying systems have the ability to enhance the oral bioavailability and solubility of lipophilic drugs. Conclusion: This technique offers further advantages such as bypassing the first pass metabolism via absorption of drugs through the lymphatic system, easy manufacturing, reducing enzymatic hydrolysis, inter and intra subject variability, and food effects.

The Potential Use of Cyclosporine Ultrafine Solution Pressurised Metered-Dose Inhaler in the Treatment of COVID-19 Patients

Introduction: Serious COVID-19 respiratory problems start when the virus reaches the alveolar level, where type II cells get infected and die. Therefore, virus inhibition at the alveolar level would help prevent these respiratory complications. Method: A literature search was conducted to collect physicochemical properties of small molecule compounds that could be used for the COVID-19 treatment. Compounds with a low melting point were selected along with those soluble in ethanol, hydrogen-bond donors, and acceptors. Results : There are severe acute respiratory syndrome coronavirus inhibitors with physicochemical properties suitable for the formulation as an ultrafine pressurised metered-dose inhaler (pMDI). Mycophenolic acid, Debio 025, and cyclosporine A are prime candidates among these compounds. Cyclosporine A (hereafter cyclosporine) is a potent SARS-CoV-2 inhibitor, and it has been used for the treatment of COVID-19 patients, demonstrating an improved survival rate. Also, inhalation therapy of nebulised cyclosporine was tolerated, which was used for patients with lung transplants. Finally, cyclosporine has been formulated as a solution ultrafine pMDI. Although vaccine therapy has been started in most countries, inhalation therapies with non-immunological activities could minimise the spread of the disease and be used in vaccine-hesitant individuals. Conclusion: Ultrafine pMDI formulation of cyclosporine or Debio 025 should be investigated for the inhalation therapy of COVID-19.

HPMC- A Marvel Polymer for Pharmaceutical Industry-Patent review

: At the present time, designing of defined release dosage forms, either controlled, sustained, modified, are gaining much importance. For the development of such delivery systems, proper blend of polymers is required, so that drug release occurs by polymer erosion, swelling, diffusion/dissolution. HPMC (hydroxypropyl methyl cellulose) is the most commonly used cellulosic polymer available in various grades to develop such types of systems. Depending upon the molecular weight and viscosity chosen, it can be applied for emulsification, adhesion, bonding, thickening, suspension, film forming and gelation. It consists of polymeric units linked together, which retain water, thereby acting as an excellent hydrophilic gel-forming polymer. It generally hydrates on the outer surface to form a gelatinous layer. It swells, expands upon contact with water and releases the drug in a predetermined manner initially and then forms a viscous gel to control the release further. The objective of the present review is to overview the recent patents and articles of HPMC, its properties, grades and its use in various drug delivery systems and as a binder, dispersing agent, bioavailability enhancer and as capsule forming material have been identified and reviewed.

Advanced Technologies in DNA-based Nanomedicine

: The application of nanotechnology in medicine and pharmaceutical purpose suggested a novel procedure in the nanotechnology terminology as nanomedicine. There is a wide range of applications for nanotechnology in medicine, such as the use of nanocarriers in drug delivery systems. Recently a remarkable attention to DNA has been made through its amazing functionality and its nature as a nanomaterial in biological systems. Since DNA is a biocompatible, the use of DNA as a nanomaterial in medicine has shown a great perspective of rational engineering of DNA nanostructures. According to new approaches in treatment of diseases in gene levels, gene therapy, using DNA as a nanomedicine possesses an important role in the medical sciences as the researchers published enormous papers and patents in the fields, for instance, the applications of DNA and DNA-based nanostructures as drug or gene nanocarriers, DNA-based diagnostics and DNA nanovasccines. Here, some examples of DNA-based nanomedicine in the patent frame were reviewed.

Co-crystals for Generic Pharmaceuticals: An Outlook on Solid Oral Dosage Formulations.

Co-crystal is an attractive alternative new class of solid forms because that can be engineered to have desired physicochemical properties. Co-crystals have gained considerable attention from the generic pharmaceutical industry after the USFDA released its finalized guidance in the year 2018 on the regulatory classification of co-crystals. In this review, we discussed how co-crystals can be explored as a potential alternative solid form for the development of a generic product that meets the legal, regulatory, and bioequivalence requirements. In the contents, we discussed in detail concepts such as the selection of coformers, various ways of making co-crystals, the strategy of characterization to discriminate between co-crystal and salt, polymorphism in co-crystals, the aspects of intellectual property and, finally, the regulatory aspects of co-crystals.