Determination of Alteration in Micromeritic Properties of a Solid Dispersion: Brunauer-Emmett-Teller Based Adsorption and Other Structured Approaches.

The present study is focused on the use of solid dispersion technology to triumph over the solubility-related problems of bexarotene which is currently used for treating various types of cancer and has shown potential inhibitory action on COVID-19 main protease and human ACE2 receptors. It is based on comparison of green locust bean gum and synthetic poloxamer as polymers using extensive mechanistic methods to explore the mechanism behind solubility enhancement and to find suitable concentration of drug to polymer ratio to prepare porous 3rd generation solid dispersion. The prepared solid dispersions were characterized using different studies like X-ray diffraction (XRD), thermal gravimetric analysis (TGA), scanning electron microscopy (SEM), Brunauer-Emmett-Teller (BET), differential scanning calorimetry (DSC), and particle size analysis in order to determine the exact changes occurred in the product which are responsible for enhancing solubility profiles of an insoluble drug. The results showed different profiles for particle size, solubility, dissolution rate, porosity, BET, and Langmuir specific surface area of prepared solid dispersions by using different polymers. In addition to the comparison of polymers, the BET analysis deeply explored the changes occurred in all dispersions when the concentration of polymer was increased. The optimized solid dispersion prepared with MLBG using lyophilization technique showed reduced particle size of 745.7±4.4 nm, utmost solubility of 63.97%, pore size of 211.597 Å, BET and Langmuir specific surface area of 5.6413 m2/g and 8.2757 m2/g, respectively.

A Mechanistic Study to Determine the Structural Similarities Between Artificial Membrane Strat-M™ and Biological Membranes and Its Application to Carry Out Skin Permeation Study of Amphotericin B Nanoformulations.

Type of biological membrane used in skin permeation experiment significantly affects skin permeation and deposition potential of tested formulations. In this study, a comparative study has been carried out to evaluate the potential of a synthetic membrane (Strat-M™) with rat, human, and porcine ear skin to carry out skin permeation study of nanoformulations of a high molecular weight drug, amphotericin B. Results demonstrated that the permeation of this high molecular weight drug through Strat-M™ showed close similitude to human skin. Value of correlation coefficient (R2) of log diffusion between Strat-M™ and human skin was found to be 0.99 which demonstrated the similarities of Strat-M™ membrane to the human skin. In similarity factor analysis, the value of f2 was also found to be 85, which further demonstrated the similarities of Strat-M™ membrane to human skin. Moreover, scanning electron microscopy (SEM), transmission electron microscopy (TEM), and Brunauer-Emmett-Teller (BET) analysis of synthetic and biological membranes depicted almost similar morphological features (thickness, pore size, surface morphology, and diameter) of synthetic membrane with human skin. The results of the study demonstrated Strat-M™ as a better alternative to carry out skin permeation experiment due to the consistent results, reproducibility, easy availability, and minimum variability with human skin.

Nanoethosomal formulation for skin targeting of amphotericin B: an in vitro and in vivo assessment.

The present study is envisaged to develop nanoethosomal formulation for enhanced topical delivery of amphotericin B (AmB) for the treatment of cutaneous fungal infections. AmB encapsulated nanoethosomes were prepared using mechanical dispersion method in a strength of 0.1% w/w similar to the strength of marketed topical formulation. Vesicle size of nanoethosomal formulations was found to be in the range of 186 ± 2 to 298 ± 4 nm. The optimized nanoethosomal formulation was further incorporated in gel base to form AmB nanoethogel formulation. Rheological characterization study of nanoethogel demonstrated its viscoelastic nature with high elasticity and resistance to deformation at 37 °C. The yield stress value was found to be 108.05 ± 2.4 and 52.15 ± 0.9 Pa for nanoethogel and marketed gel formulation, respectively. The nanoethogel formulation exhibited 2.7- and 3.5-fold higher steady state transdermal flux and skin deposition of AmB, respectively, in comparison to marketed formulation. Confocal laser scanning microscopy (CLSM) study also revealed enhanced skin permeation and deposition with nanoethogel formulation. In vivo study showed that topical application of nanoethogel does not exhibit any skin irritation as tested by Draize test. The developed formulation, in comparison to the marketed gel, demonstrated a remarkable increase in the antifungal activity against Candida albicans. It is thus corroborated from the above results that nanoethosomal formulation represents an efficacious carrier for effective topical delivery of AmB.

A Unique Case of Late Presentation Giant Lower Extremity Malignant Melanoma.

This case describes a unique presentation of a rare malignancy: giant melanoma. Due to the accessibility of healthcare in the United States, it is unusual for melanomas to grow to massive sizes without clinical intervention. In fact, an in-depth literature review elicited only a handful of similar cases. Giant malignant melanomas are typically defined by a cutoff size of no less than 10 cm in diameter. They often present with distant metastases and are highly invasive. Due to limited yet highly variable presentations, there is no standardized approach to treating this class of melanomas. We present a case with unique features not previously documented in similar cases that was ultimately treated with a novel approach.

Nanotechnology-based Herbal Formulations: A Survey of Recent Patents, Advancements, and Transformative Headways.

Nanotechnology in association with herbal medicine can lead to enhanced therapeutic and diminished adverse effects of medication. In turn, it can lead to synergistic effects of administered compound overcoming its demerits. Nowadays, the trend of herbal compounds to treat even a small illness is gaining momentum. Gone are the days when the ineffectiveness of a compound was impossible to be dealt with. Nevertheless, in this competitive era of science and innovative technology, it has become possible to maximize the usefulness of ineffective yet potent herbal compounds. The demand for herbal compounds is getting amplified because of their ability to treat a myriad of diseases, including COVID-19, showing fewer side effects. The merger of nanotechnology with traditional medicine augments the potential of herbal drugs for devastating dangerous and chronic diseases like cancer. In this review article, we have tried to assimilate the complete information regarding the use of different nanocarriers to overcome the drawbacks of herbal compounds. In addition, all the recent advancements in the herbal field, as well as the future exploration to be emphasized, have been discussed.

Double carbapenem regimen used as salvage therapy to treat multidrug-resistant Klebsiella pneumoniae causing ventilator-associated pneumonia.

Carbapenemase-producing Klebsiella pneumoniae is an emerging threat worldwide. The appropriate therapy for infections due to these multidrug-resistant pathogens is not well defined and depends upon the susceptibilities of individual isolates, and the choices are often severely limited. We report a case of a 8-year-old male child with ARDS with left-sided tubercular pleural effusion who developed ventilator-associated pneumonia due to multidrug-resistant Klebsiella pneumoniae treated successfully with a regimen comprising a combination of colistin and double carbapenem.

Multipotentiality of Luliconazole against Various Fungal Strains: Novel Topical Formulations and Patent Review.

Luliconazole is a broad-spectrum antifungal agent with impactful fungicidal and fungistatic activity. It has shown exceptional potency against miscellaneous fungal strains like Candida, Aspergillus, Malassezia, Fusarium species and various dermatophytes. Luliconazole belongs to class II of the Biopharmaceutical Classification System with low aqueous solubility. Although it is available conventionally as 1% w/v topical cream, it has limitations of lower skin permeation and shorter skin retention. Therefore, nanoformulations based on various polymers and nanostructure carriers can be employed to overcome the impediments regarding topical delivery and efficacy of luliconazole. In this review, we have tried to provide insight into the literature gathered from authentic web resources and research articles regarding recent research conducted on the subject of formulation development, patents, and future research requisites of luliconazole. Nanoformulations can play a fundamental role in improving topical delivery by escalating dermal localization and skin penetration. Fabricating luliconazole into nanoformulations can overcome the drawbacks and can efficiently enhance its antimycotic activity. It has been concluded that luliconazole has exceptional potential in the treatment of various fungal infections, and therefore, it should be exploited to its maximum for its innovative application in the field of mycology.

Investigation of antiplasmodial efficacy of lupeol and ursolic acid isolated from Ficus benjamina leaves extract.

This study emphasizes on the investigation of antiplasmodial activity of triterpenoids isolated from Ficus benjamina leaves. An unsaponified fraction of petroleum ether extract of plant leaves was subjected to silica gel column chromatography which led to the isolation of two known triterpenoids; namely ursolic acid and lupeol. These compounds were evaluated for antiplasmodial activity by schizont maturation inhibition assay using 3D7 Plasmodium strains. Both, ursolic acid and lupeol were found to exhibit significant antiplasmodial effect with an IC50 value of 18 µg/ml and 3.8 µg/ml, respectively. This study further confirms the traditional role of Ficus benjamina plant in the treatment of malaria which may be attributed to ursolic acid and lupeol.

Safe and Effective Delivery of Amphotericin B: A Survey of Patents.

BACKGROUND: Amphotericin B, designated as the gold standard among antifungal drugs is the only fungicidal effective against systemic fungal infections. But this drug has various pitfalls associated with it, to bypass which various techniques have been employed and resulted in a variety of lipid based commercially available formulations, which demolished only few of the shortcomings associated with this drug. Further, improvement in the delivery systems of Amphotericin B is advancing at increasingly frenetic pace, to surmount its research and to exploit its therapeutic potency with least toxicities. METHOD: The patent search on "Amphotericin B for its safe and effective delivery" has been carried out to present assimilated information on the patents of the universally accepted Amphotericin B formulations and technologies. Also, the area of focus was the physicochemical properties of Amphotericin B, their role in formulation development and also nanotechnology based formulations of Amphotericin B. RESULTS: Amphotericin B possesses poor aqueous solubility and systemic toxicity rendering obstacle in its formulation development. The interest of scientists and pharmaceutical industries to make further investments in the development of Amphotericin B formulations is due to rare occurrence of resistance to this drug. To bypass these drawbacks, various techniques have been patented which resulted in a variety of commercially available formulations to overcome the limitations of high cost, limited availability, poor storage stability and poor patient compliance. In lieu to this, scientists have developed and patented many novel drug delivery system based formulations and technologies such as use of novel carriers, modification in process for production and purification of Amphotericin B, formation of salts and complexes etc. to bring in limelight the benefits of this wonder drug. CONCLUSION: The purpose of the article is to present assimilated information regarding patents on Amphotericin B formulations and technologies.