Scrutinizing the Feasibility of Nonionic Surfactants to Form Isotropic Bicelles of Curcumin: a Potential Antiviral Candidate Against COVID-19

Investigating bicelles as an oral drug delivery system and exploiting their structural benefits can pave the way to formulate hydrophobic drugs and potentiate their activity. Herein, the ability of non-ionic surfactants (labrasol®, tween 80, cremophore EL and pluronic F127) to form curcumin loaded bicelles with phosphatidylcholine, utilizing a simple method, was investigated. Molecular docking was used to understand the mechanism of bicelles formation. The % transmittance and TEM exhibited bicelles formation with labrasol® and tween 80, while cremophor EL and pluronic F127 tended to form mixed micelles. The surfactant-based nanostructures significantly improved curcumin dissolution (99.2 ± 2.6% within 10 min in case of tween 80-based bicelles) compared to liposomes and curcumin suspension in non-sink conditions. The prepared formulations improved curcumin ex vivo permeation over liposomes and drug suspension. Further, the therapeutic antiviral activity of the formulated curcumin against SARS-CoV-2 was potentiated over drug suspension. Although both Labrasol® and tween 80 bicelles could form bicelles and enhance the oral delivery of curcumin when compared to liposomes and drug suspension, the mixed micelles formulations depicted superiority than bicelles formulations. Our findings provide promising formulations that can be utilized for further preclinical and clinical studies of curcumin as an antiviral therapy for COVID-19 patients.

Niosomes: A Promising Novel Nano Carrier for Drug Delivery

Niosomes are vesicles, which are formulated by hydrating the mixture of cholesterol, non-ionic surfactant and other biodegradable lipids. Niosomes increase the drug activity as compare to their conventional dosage form of a drug. Niosomes can be used as carrier of amphiphilic and lipophilic drugs. Niosomes may overcome the issues related to instability, fast degradation, low bioavailability, and insolubility of medications. The structure of niosomes either multilamellar or unilamellar, is depends on the method of formulation. Niosomes contain very efficient drug delivery potential for site-specific delivery of anti-cancer, anti-infective agents, etc. Niosomes are stable as well as cost effective carriers as compared with other drug formulations. Niosomes also have various applications in parental drug delivery system, topical drug delivery system, oral drug delivery system and novel drug delivery system such as targeted drug delivery system and controlled drug release system.

Preparation and Evaluation of a Novel Oral Microemulsion Drug Delivery System for Enhancing the Bioavailability of Diltiazem

Diltiazem, a calcium ion cellular influx inhibitor is known for its limited and variable bioavailability. This study is intended to explore the benefits of microemulsion formulation as an oral drug delivery system for immediate release to improve the bioavailability and efficacy of Diltiazem. Methods: Oil in water microemulsion was prepared using the simple water titration method. The optimized formulation was evaluated for physicochemical parameters like viscosity, pH, conductivity, and accelerated stability studies. In vitro release, diltiazem microemulsion was investigated.

FORMULATION AND EVALUATION OF FLOATING IN SITU GEL OF OMEPRAZOLE MAGNESIUM FOR ORAL DRUG DELIVERY SYSTEM

Objective: Omeprazole magnesium is indicated for the treatment of erosive esophagitis associated with gastroesophageal reflux disease. It is one of the highly prescribed proton pump inhibitor in the management of peptic ulcer diseases. The therapeutic concentration of a drug in blood can be maintained for a prolonged period of time by administering it in the form of in situ floating gel dosage form. Omeprazole magnesium undergoes degradation at a low pH of the esophagus and stomach; it is therefore given as in situ gel, so, there is minimum contact with acidic pH. Methods: Omeprazole magnesium suspension prepared using various polymers and floating agents in varying concentrations. Several evaluation tests including dissolution test to ensure the release of the drug from formulation by in vitro technique, color and homogeneity, in vitro floating duration, in vitro gelling capacity, drug content determination, pH of the formulation, and floating lag time were studied. Results: All formulations demonstrated good Fourier-transform infrared compliance and no interaction between drug, polymer, and other excipients. The study’s findings show that the formulation F6 showed the best results. Conclusion: The developed formulation was a viable alternative conventional solution by virtue of its ability to enhance bioavailability through its longer gastric residence time and ability to sustain drug release as well as the advantage of floating and pH which minimize the degradation of omeprazole magnesium which is easily degraded by acidic environment.

Oral GLP-1 Analogue Ameliorates Obesity-Induced Diabetes In Db/Db Mouse

Type 2 diabetes is currently experiencing an outbreak worldwide. GLP-1 effectively lowers blood glucose level as an emerging target for the treatment of type 2 diabetes. However, the application of GLP-1 is limited by short half-life and too expensive cost in clinic. In this study we employed the food-grade probiotics as delivery system to express human GLP-1 and its analogue. Recombinant lactococcus lactis could express GLP-1 and analogue in vitro and modified GLP-1 analogue was more resistant to DPP-4 degradation. Oral administration of GLP-1 analogue could reduce the fat mass. More importantly, GLP-1 analogue improved hyperglycemia and insulin resistance in Db/Db mouse although the insulin secretion is not observed in vitro. Our study demonstrates that lactococcus lactis genetically modified with single amino acid mutation could prolong half-life of GLP-1 and increase insulin sensitivity in Db/Db mouse model as an oral drug delivery system driving the development and innovation of drug therapy for type 2 diabetes.

A Comprehensive Review On Pelletization Technology: A Novel Strategy For Formulation Development

Pelletization technology is gaining very much attention in present times as it has provided a competent pathway for the oral drug delivery system manufacturing. Pellets offers many biopharmaceuticals as well as technological recompenses over the conventional dosage forms. Pellets offer required strength for dose which can be blended for the delivery of incompatible bioactive agents and helps in providing different release profiles. In this review we will be discussing the extensively used techniques of pelletization, extrusion and spheronization in detail with their methods and applications in the field of pharmacy as a competent pathway for the novel drug delivery systems.

Evaluation of Ibuprofen/Montmorillonite Nano-Clay Composites as an Oral Drug Delivery System and In-Vitro Drug Release Performance

A formulation for controlled delivery of ibuprofen (IBU) involving montmorillonite (MMT) nanoclays has been proposed. The present work has investigated the beneficial effect of MMT in improving controlled delivery of IBU. The intercalation of IBU into the interlayer of MMT was studied under different processing conditions such as reaction time and initial concentration of IBU. To characterize the IBU/MMT composites, X-ray diffraction (XRD) and Fourier transform infrared spectra (FTIR) were performed. The release behavior of IBU from IBU/MMT composites have been investigated under vitro conditions using buffer media of simulated gastric fluid (pH 1.2) and simulated intestinal fluid (pH 7.4) at 37 °C. Controlled release of IBU from IBU/MMT composite has been observed during in vitro release experiments. Different mathematical models were used for fitting our experimental results, among them the best fitting was found for Higuchi equation based on the parabolic diffusion process.