Drug Delivery Letters - Volume 12, Issue 4, 2022

Background: During the development of the new formulations, the hydrophobic drugs face many problems leading to poor water solubility and problems related to bioavailability. Topical drug delivery is a popular and unique process that directs the action of various drugs on the skin for the treatment and diagnosis of various diseases and disorders such as urticaria, inflammation, rheumatism, etc. This topical release system is usually used to escape the first-pass metabolism. An emulgel is a superior formulation with combined advantages of both an emulsion and agel. Gel preparations normally offer earlier drug release than other predictable ointments and creams. Objective: The main aim of this review is to deal with the problems associated with the delivery of hydrophobic drugs and to tackle these problems using an emulgel formulation. Emulgel mainly provides better stability, prolonged local contact, controlled release of drugs with short half-life, and better loading capacity. Methods: The review was extracted from the searches performed in PubMed, Google Patents, Medline, and Google Scholars, etc. Data from these searches were collected and evaluated to get information about the available literature on the emulgel formulation. The literature obtained was studied thoroughly as per the requirement of the objective of this review. Results: The details of the emulgel formulation, the advantages and disadvantages associated with it, and the methods for characterization of the formulation are compiled here in this review. Along with this, some reported patents have also been included in this review to conclude the future of emulgel formulation in topical drug delivery. Conclusion: Emulgel is becoming very popular as a drug delivery system to deliver many antifungal, analgesics, anti-acne, anti-inflammatory drugs, and a number of cosmetics with a wide scope to be explored further. This review article is motivated by the formulation, characterization, patents, and biological activities of emulgel formulation.

Background: Cancer is a leading cause of mortality. A vast number of conventional chemotherapeutic agents are being used to treat cancer; however, these conventional chemotherapeutic agents kill both tumor and healthy cells. Introduction: Cancer immunotherapy has gained tremendous attention and is being researched today to treat cancer. In the case of immunotherapy, the therapeutic techniques target only cancer cells. This therapy has very less side effects compared to conventional chemotherapeutic agents. Nowadays, dendrimers as nanosystem carriers play a very crucial role in the field of immunotherapy. Methods: Biomaterials such as poly(glycerol), PAMAM, carbohydrate-derived citric acid polyester (PGLSA-OH), polyethylene glycol (PEG), poly(propylene imine) (PPI), melamine, triagine, and phosphorhydrazone have been reported for the production of dendrimers. Dendritic-based nonocarriers are classified according to the size of the dendrimers moiety and their generation. They are also classified based on the presence of internal layers of dynamic dendritic scaffolds that interact with the drugs non-covalently. Results: Dendrimers are being researched to deliver DNA drugs for antisense therapy. In certain circumstances, dendrimers like PPI or PAMAM have been employed to deliver non-viral genes. Dendrimers can interact with various forms of nucleic acids such as plasmid DNA, antisense oligonucleotides, and RNA to form complexes that protect the nucleic acid from degradation. Conclusion: Dendrimers are promising candidates for improving the solubility and diminishing the toxic effect of anticancer drugs as well as for targeted delivery to cancer cells. Different types of dendrimers such as PAMAM-PEG dendrimers, triazine dendrimers, glycodendrimers, phosphorus dendrimers, and carbosilaneden dendrimers are being explored for commercial applications for cancer therapy, and so far, they have produced encouraging results.

Background: The pulmonary route of administration has shown viability and effectiveness in local and systemic delivery, as a non-invasive method, not only for active pharmaceutical ingredients but also for genes, proteins, and enzymes for pulmonary and non-pulmonary diseases. Objectives: Nanoparticulate systems such as liposomes, solid lipid nanoparticles, nanostructured lipid carriers, emulsions, nanosuspensions, polymeric nanoparticles, and metal-based have been investigated as delivery carriers for the lungs. Nanoparticulate drug delivery systems are known for their optimum small size and suitability for pulmonary absorption as it is well recognized that drug particles within the size range of 1-5 μm are the best for pulmonary deposition. Results: The advantages of these colloidal systems are generated by their small size, large surface area, and rapid absorption. These systems are characterized by ease of preparation as inhalable formulation, the ability to increase drug concentration at the site of disease, preventing and minimizing drug loss and degradation, and the possibility of cell targeting. Conclusion: This article provides a brief review of the features of different aerosol devices, their advantages, limitations, and methods utilized for particle size analysis with a focus on the emerging field of nanocarriers as vehicles for pulmonary delivery for various lung disorders.

Objective: The present study was designed to isolate, characterize, formulate, and evaluate the disintegration properties of banana starch in dispersible Lornoxicam tablet formulation. Methods: The alkaline extraction method used sodium hydroxide as a lye solution to isolate starch from unripe banana fruit. Starch was subjected to characterization for physicochemical properties, viscosity and flow properties, Fourier-transform infrared spectroscopy (FTIR) scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and X-ray crystallography (XRD) study. Flow properties of starch were determined as per the standard procedure. Tablets were formulated by a wet granulation method using starch as a disintegrant, and the in-vitro release characteristic of the prepared tablets was analyzed. Different concentrations of isolated starch were studied for disintegrating properties compared to corn starch. Results: Studies indicate that starch obtained is qualitatively and quantitatively comparable to corn starch. SEM, FTIR, DSC and XRD data confirmed the polysaccharide nature of the starch. The physicochemical properties of starch passed the prescribed evaluation tests for tablets. These tablets also confirmed the disintegration and dissolution specifications as per Indian Pharmacopoeia. Conclusion: From the above study, it can be concluded that starch obtained from banana shows qualitatively and quantitatively good disintegration characteristics compared to corn starch. These tablets also confirmed a significant degree of dissolution as per the standards. Evaluations also specified that banana starch possesses acceptable disintegrating characteristics compared to corn starch and can be used as a disintegrant in tablet formulation.

Background: Microspheres are controlled drug delivery systems (CDDS) due to their potential to encapsulate various drugs, nucleic acids, and proteins. Their benefits include greater biocompatibility, increased bioavailability, and controlled release. Presently, existing antiulcer agents suffer from severe side effects, which has restricted their utility and encouraged the requirement of a harmless and proficient new antiulcer agent. The rationale of the present research work was to improve the absorption of the drug in the stomach for better anti-ulcer action and fewer side effects. Objective: This study aimed to prepare and examine floating microspheres using berberine hydrochloride to increase gastric retention without interacting with the mucosa inside the stomach. Methods: The capillary extrusion technique was used with the aid of chitosan, a polymer, in addition to sodium lauryl sulphate, a crosslinking agent. Scanning electron microscopy characterized the surface morphology of the prepared microspheres. The effects of polymeric concentration as well as the concentration of cross-link agent on percent yield, in vitro floating behavior, and in vitro drug release were efficiently assessed. Results: The drug follows a mechanism for prolonged release, known as diffusion. Prolonged drug release (12 hrs) was seen in the prepared microspheres, and they also remained buoyant for around 10 hrs. In vivo evaluation study was successfully performed. From the values of ulcer indexes for various groups, percentage protection was determined. The treatment group (F-2 formulation) showed maximum percentage protection of 97.29%. Conclusion: The prepared floating microspheres can make potential candidates adaptable to any intra- gastric conditions for multiple-unit delivery devices.

Background: Amidst levodopa being considered as the “Gold standard” in the treatment of Parkinson’s disease (PD), it still has critical therapeutic issues with its dose regimen and dosage forms leading to severe adverse drug effects, decreased drug efficacy during chronic use, and requires an enforced “drug holiday” in PD patients. Hence, in this study, we designed a novel levodopa and carbidopa water-in-oil-in-water (w/o/w) formulation for bioavailability improvement in the central nervous system (CNS). Methods: The new one-in-one embedment of the w/o/w levodopa and carbidopa emulsion formulation was obtained by a double emulsion technique. The plasma and brain levels following intravenous administration of the emulsions in rats were determined. Results: The incorporation of stearylamine (a cationic surfactant) considerably increased the surface charge density of the emulsion droplets. This formulation exhibited a narrow particle size distribution enabling parenteral administration. The formulation also provided a high drug loading capacity. In in vivo study, this novel formulation significantly increased the bioavailability of levodopa in the CNS (P < 0.001). The strong resistance to desorption (due to higher charge density) and the presence of positive charge on the particles upon dilution may be the main reason for enhanced brain levels of levodopa. Conclusion: Our current formulation F5 may decrease the dose of levodopa, leading to decreased adverse effects and dosing problems, thus appreciably benefit PD patients in the future.