Development and Evaluation of PEG-gelatin-based Microparticles to Enhance the Oral Delivery of Insulin.

Background: Diabetes mellitus is a global disease identified by hyperglycemia due to defects in insulin secretion, insulin action, or both.

Objective: The main objective of this research was to evaluate the ability of gelatinized Poly(ethylene glycol) (PEG) microparticles to be used as carriers for oral insulin delivery via double emulsion preparation.

Methods: Five different batches of the formulation consisting of gelatin:PEG were prepared as follows: 0:1 (W1), 1:0 (W2), 1:1 (W3), 1:3 (W4), and 3:1 (W5).

Retraction notice to "Mechanistic insight into the bioactivity of prodigiosin-entrapped lipid nanoparticles against triple-negative breast, lung and colon cancer cell lines" [Heliyon 9 (2023) e16963].

[This retracts the article DOI: 10.1016/j.heliyon.

Formulation and Evaluation of Gum-based Mucoadhesive Sustained-release Matrix Tablets of Diclofenac Sodium.

Objective: This study aimed to evaluate gum (CAG) for the formulation of mucoadhesive sustained-release matrix tablets of diclofenac sodium.

Methods: Different batches of granules containing CAG and 100 mg of DS in ratios 0.5:1, 1:1, 2:1, and 3:1 were prepared, compressed into tablets, and evaluated for mucoadhesive strength, swelling index, and drug release in SGF (pH 1.

Mechanistic insight into the bioactivity of prodigiosin-entrapped lipid nanoparticles against triple-negative breast, lung and colon cancer cell lines.

This research investigates the potentials of prodigiosinPG derived from bacteria and its formulations against triplenegative breast (TNB), lung, and colon cancer cells. The PG was extracted from using continuous batch culture, characterized, and formulated into lyophilized parenteral nanoparticles (PNPs). The formulations were characterized with respect to entrapment efficiency (EE), DSC, FT-IR, TEM, and proton nuclear magnetic resonance (1H NMR) spectroscopy.

Exploitation of capsule system for colon targeted drug delivery of biopolymer-based microparticles: and applications.

The current study was to improve and control aceclofenac delivery prepared as biopolymer-based microparticles for effective colon-targeted drug delivery using modified gelatin capsules (MGCs) at different time intervals developed in two batches (C1 and C2). Microparticles were formulated with extracted mucuna gum using liquid paraffin oil (AC.LPO) and soybean oil (AC.

Enhanced circulation longevity and pharmacodynamics of metformin from surface-modified nanostructured lipid carriers based on solidified reverse micellar solutions.

Metformin hydrochloride (MTH) has been associated with poor/incomplete absorption (50-60%), low bioavailability, short half-life (0.4-0.5 h), high dosage and dose-related side effects.

Improved antimalarial activity of caprol-based nanostructured lipid carriers encapsulating artemether-lumefantrine for oral administration.

Background: Artemether and lumefantrine display low aqueous solubility leading to poor release profile; hence the need for the use of lipid-based systems to improve their oral bioavailability so as to improve their therapeutic efficacy.

Aim And Objective: The objective of this work was to utilize potentials of nanostructured lipid carriers (NLCs) for improvement of the oral bioavailability of artemether and lumefantrine combination and to evaluate its efficacy in the treatment of malaria. This study reports a method of formulation, characterization and evaluation of the therapeutic efficacies of caprol-based NLC delivery systems with artemether and lumefantrine.

Development of lipid-based microsuspensions for improved ophthalmic delivery of gentamicin sulphate.

Anterior eye segment disorders are treated with eye drops and ointments, which have low ocular bioavailability necessitating the need for improved alternatives. Lipid microsuspension of gentamicin sulphate was developed for the treatment of susceptible eye diseases. Lipid microsuspensions encapsulating gentamicin sulphate were produced by hot homogenization and evaluated.

Formulation and evaluation of transdermal nanogel for delivery of artemether.

Artemether (ART) is second to artesunate in being the most widely used derivatives of artemisinin in combination therapy of malaria. Nanostructured lipid carrier (NLC) formulations were prepared following our previous report using optimized ART concentration of 0.25 g dissolved in 5% w/v mixture of solid (Gelucire 43/01 and Phospholipon 85G) and liquid (Transcutol) lipids at 90 °C.

Biodegradable nanoparticles from prosopisylated cellulose as a platform for enhanced oral bioavailability of poorly water-soluble drugs.

Bio-inspired nanotechnology-based strategies are potential platforms for enhanced dissolution and oral biovailability of poorly water-soluble drugs. In this study, a recently patented green biopolymer (Prosopis africana gum, PG) was compatibilized with microcrystalline cellulose (MCC), a conventional polysaccharide, via thermo-regulated coacervation to obtain PG-MCC (1:0, 1:1, 1:2, 2:1, and 0:1) rational blends and the nanoparticles developed with optimized (1:1) biocomposites (termed "prosopisylated cellulose") by combined homogenization-nanoprecipitation technique was engineered as a high circulating system for improved oral bioavailability of griseofulvin (GF), a model Biopharmaceutics Classification System (BCS) Class-II drug. The effects of biopolymer interaction on morphological and microstructural properties of drug-free biocomposites obtained were investigated by Fourier transform infra-red spectroscopy, scanning electron microscopy and x-ray diffractometry, while the physicochemical properties and in-vivo pharmacokinetics of GF-loaded nanoparticles were also ascertained.

Insulin-loaded mucoadhesive nanoparticles based on mucin-chitosan complexes for oral delivery and diabetes treatment.

In this study, insulin-loaded nanoparticles (NPs) were prepared via self-gelation method using chitosan and aqueous soluble snail mucin as natural polymers. Herein, mucins were ionically interacted with chitosan at different concentrations to obtained insulin-loaded NPs, labelled as A1 (1:1) (i.e.

A new lipid-based oral delivery system of erythromycin for prolong sustain release activity.

Erythromycin-loaded solid lipid microparticles (SLM) based on solidified reverse micellar solution (SRMS) as an oral delivery formulation was studied. Hot homogenization technique was employed to prepare erythromycin stearate-loaded SLMs using blends of Softisan® 154 and Phospholipon® 90H or beeswax in the ratio of 1:2, and characterized in vitro. Antibacterial evaluation of the formulations was carried out by agar diffusion technique against some selected clinical isolates of bacterial.

Novel Intravaginal Drug Delivery System Based on Molecularly PEGylated Lipid Matrices for Improved Antifungal Activity of Miconazole Nitrate.

The aim of this study was to investigate the potential of microparticles based on biocompatible phytolipids [Softisan® 154 (SF) (hydrogenated palm oil) and super-refined sunseed oil (SO)] and polyethylene glycol- (PEG-) 4000 to improve intravaginal delivery of miconazole nitrate (MN) for effective treatment of vulvovaginal candidiasis (VVC). Lipid matrices (LMs) consisting of rational blends of SF and SO with or without PEG-4000 were prepared by fusion and characterized and employed to formulate MN-loaded solid lipid microparticles (SLMs) by melt-homogenization. The SLMs were characterized for physicochemical properties, anticandidal activity, and stability.

Surface-modified mucoadhesive microgels as a controlled release system for miconazole nitrate to improve localized treatment of vulvovaginal candidiasis.

The use of conventional vaginal formulations of miconazole nitrate (MN) in the treatment of deep-seated VVC (vulvovaginal candidiasis) is limited by poor penetration capacity and low solubility of MN, short residence time and irritation at the application site. Surface-modified mucoadhesive microgels were developed to minimize local irritation, enhance penetration capacity and solubility and prolong localized vaginal delivery of MN for effective treatment of deep-seated VVC. Solid lipid microparticles (SLMs) were prepared from matrices consisting of hydrogenated palm oil (Softisan® 154, SF) and super-refined sunseed oil (SO) with or without polyethylene glycol (PEG)-4000, characterized for physicochemical performance and used to prepare mucoadhesive microgels (MMs) encapsulating MN, employing Polycarbophil as bioadhesive polymer.

Novel solidified reverse micellar solution-based mucoadhesive nano lipid gels encapsulating miconazole nitrate-loaded nanoparticles for improved treatment of oropharyngeal candidiasis.

Objective: To develop and evaluate solidified-reverse-micellar-solution (SRMS)-based oromucosal nano lipid gels for improved localised delivery of miconazole nitrate (MN).

Methods: Phospholipon 90G and Softisan 154 (3:7) were used to prepare SRMS by fusion. Solid lipid nanoparticles (SLNs, 0.

Sustained-release liquisolid compact tablets containing artemether-lumefantrine as alternate-day regimen for malaria treatment to improve patient compliance.

The present study aimed to develop low-dose liquisolid tablets of two antimalarial drugs artemether-lumefantrine (AL) from a nanostructured lipid carrier (NLC) of lumefantrine (LUM) and estimate the potential of AL as an oral delivery system in malariogenic Wistar mice. LUM-NLCs were prepared by hot homogenization using Precirol ATO 5/Transcutol HP and tallow fat/Transcutol HP optimized systems containing 3:1 ratios of the lipids, respectively, as the matrices. LUM-NLC characteristics, including morphology, particle size, zeta potential, encapsulation efficiency, yield, pH-dependent stability, and interaction studies, were investigated.

Improved dissolution and anti-inflammatory activity of ibuprofen-polyethylene glycol 8000 solid dispersion systems.

Background: The purpose of this study was to develop ibuprofen (IB)-polyethylene glycol (PEG) 8000 solid dispersions (SDs) and investigate them for in vitro dissolution and in vivo anti-inflammatory activity.

Materials And Methods: IB-PEG 8000 SDs were prepared by fusion method using varying combination ratios of IB and PEG 8000. Characterization based on surface morphology, particle size, absolute drug content, and Fourier transform infrared (FT-IR) spectroscopy was carried out on the SDs.

Formulation, characterization and evaluation of the effect of polymer concentration on the release behavior of insulin-loaded Eudragit(®)-entrapped mucoadhesive microspheres.

Introduction: The aim of this study was to use Eudragit(®) RL 100 (pH-independent polymer) and magnesium stearate (a hydrophobic droplet stabilizer) in combination to improve the controlled release effect of insulin-loaded Eudragit(®) entrapped microspheres prepared by the emulsification-coacervation technique.

Materials And Methods: Mucoadhesive insulin-loaded microspheres containing magnesium stearate and varying proportions of Eudragit(®) RL 100 were prepared by the emulsification-coacervation technique and evaluated for thermal properties, physicochemical performance, and in vitro dissolution in acidic and subsequently basic media.

Results: Stable, spherical, brownish, discrete, free-flowing and mucoadhesive insulin-loaded microspheres with size range of 14.

Investigation of novel solid lipid microparticles based on homolipids from Bos indicus for the delivery of gentamicin.

Background: The aim of this study was to formulate solidified reverse micellar solution (SRMS)-based solid lipid microparticles (SLMs) using homolipids from tallow fat (Bos indicus) and evaluate its potential for enhanced delivery of gentamicin.

Materials And Methods: SLMs were formulated by melt-emulsification using SRMS (15% w/w Phospholipon(®) 90G in 35% w/w Bos indicus), polyethylene glycol 4000 (PEG) and gentamicin (1.0, 2.

Formulation and characterization of hydrochlorothiazide solid lipid microparticles based on lipid matrices of Irvingia fat.

Introduction: The purpose of this study was to improve the solubilization, bioavailability, and permeability of hydrochlorothiazide (HCTZ) by the formulation and characterization of HCTZ solid lipid microparticles (SLMs) based on fat derived from Irvingia gabonensis var. excelsa (Irvingia wombolu) and Phospholipon(®)90G (P90G).

Materials And Methods: Irvingia fat was extracted from the nut of I.

Formulation, in vitro and in vivo evaluation of halofantrine-loaded solid lipid microparticles.

Context: Formulation, characterization, in vitro and in vivo evaluation of halofantrine-loaded solid lipid microparticles (SLMs).

Objective: The objective of the study was to formulate and evaluate halofantrine-loaded SLMs.

Materials And Methods: Formulations of halofantrine-loaded SLMs were prepared by hot homogenization and thereafter lyophilized and characterized using particle size, pH stability, loading capacity (LC) and encapsulation efficiency (EE).

Solid lipid micro-dispersions (SLMs) based on PEGylated solidified reverse micellar solutions (SRMS): a novel carrier system for gentamicin.

The purpose of this study was to formulate and evaluate novel PEGylated solidified reverse micellar solutions (SRMS)-based solid lipid microparticles (SLMs) for improved delivery of gentamicin. Lipid matrix (SRMS) [consisting of 15% w/w Phospholipon® 90G (P90G) in 35% w/w dika wax (Irvingia gabonensis) was formulated and characterized by differential scanning calorimetry (DSC). SLMs were formulated by melt-emulsification using the SRMS, PEG 4000 and gentamicin (1.

Influence of magnesium stearate on the physicochemical and pharmacodynamic characteristics of insulin-loaded Eudragit entrapped mucoadhesive microspheres.

Effective oral insulin delivery has remained a challenge to the pharmaceutical industry. This study was designed to evaluate the effect of magnesium stearate on the properties of insulin-loaded Eudragit® RL 100 entrapped mucoadhesive microspheres. Microspheres containing Eudragit® RL 100, insulin, and varying concentrations of magnesium stearate (agglomeration-preventing agent) were prepared by emulsification-coacervation method and characterized with respect to differential scanning calorimetry (DSC), morphology, particle size, loading efficiency, mucoadhesive and micromeritics properties.

Design of novel miconazole nitrate transdermal films based on Eudragit RS100 and HPMC hybrids: preparation, physical characterization, in vitro and ex vivo studies.

The objective of this study was to formulate and evaluate transdermal films containing miconazole nitrate (MN), a poorly water-soluble imidazole antifungal agent, with a view to enhancing its delivery across intact skin. Transdermal films of MN were formulated by solvent casting technique using admixtures of film-forming polymers - Eudragit RS100 and hydroxypropylmethylcellulose (HPMC) (2:8, 4:6, 5:5, 6:4 and 8:2) with polyethylene glycol 8000 (plasticizer and permeation enhancer) and Tween 80 (mobile surfactant). The films were evaluated for weight uniformity, folding endurance, thickness, moisture loss and uptake, bioadhesive strength, drug content, skin irritation on rabbits and time-resolved stability.