Soft Gelatin Capsules (Softgels)

Gullapalli, Rampurna P.

doi:10.1002/jps.22151

Cited by 107 publications

(102 citation statements)

References 215 publications

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“…In addition, it can protect the encapsulated compound against oxygen and light, and it is able to readily disperse in gastric juices. From the industrial point of view, this technology is benefi cial since it minimizes potential generation of dust during manufacturing and thereby improves the safety of production personnel (17,18). Soft gels have received enormous consumer acceptance due to the ease of swallowing and unpleasant taste masking (19).…”

Section: Merivamentioning

confidence: 99%

Curcumin phytosomal softgel formulation: Development, optimization and physicochemical characterization

Allam

Abdallah

2015

Acta Pharmaceutica

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Curcumin, a naturally occurring lipophilic molecule can exert multiple and diverse bioactivities. However, its limited aqueous solubility and extensive presystemic metabolism restrict its bioavailability. Curcumin phytosomes were prepared by a simple solvent evaporation method where free fl owing powder was obtained in addition to a newly developed semisolid formulation to increase curcumin content in soft gels. Phytosomal powder was characterized in terms of drug content and zeta potential. Thirteen diff erent soft gel formulations were developed using oils such as Miglyol 812, castor oil and oleic acid, a hydrophilic vehicle such as PEG 400 and bioactive surfactants such as Cremophor EL and KLS P 124. Selected formulations were characterized in terms of curcumin in vitro dissolution. TEM analysis revealed good stability and a spherical, self-closed structure of curcumin phytosomes in complex formulations. Stability studies of chosen formulations prepared using the hydrophilic vehicle revealed a stable curcumin dissolution patt ern. In contrast, a dramatic decrease in curcumin dissolution was observed in case of phytosomes formulated in oily vehicles.Keywords: curcumin, phospholipid, phytosomes, bioavailability, lipids, soft gels INTRODUCTION Curcumin (CUR) found in the turmeric rhizomes can exert multiple and diverse bioactivities, including antioxidant, antitumor, anti-inflammatory, antidiabetic, antirheumatic, wound healing, antiviral, hepatoprotective, and anti-HIV activity (1). Despite the potential biological eff ects of CUR, poor bioavailability in both rodents and humans, as reported in several pharmacokinetic studies (2), demands high doses to reach therapeutic drug levels. Detectable serum levels were not achieved until doses of up to 3.6 g were used; consequently, a 3.6 g daily dose of oral CUR was used in the phase II clinical trial in patients with advanced colorectal cancer (3). Keeping in mind the promise of CUR as a therapeutically active agent and its poor oral absorption due to its limited aqueous solubility and extensive presystemic metabolism, it is necessary to develop a new formulation of CUR that could augment its oral absorption and enhance its therapeutic activity.To improve the bioavailability of CUR, numerous approaches and technologies have been investigated over the past decades, including the use of solid dispersion (4), copolymeric micelles (5), polymeric nanoparticles (6), lipid based nanoparticles (7), self microemulsion (8), liposomes (9) and complexation with phospholipids (10, 11). All these approaches are expected to provide bioavailability enhancement and improved absorption in the intestinal tract.Phytosomes are considered to be a safe and convenient delivery system, able to enhance oral bioavailability of poorly water soluble drugs. Their safety is related to the similarity between their structural components and the lipid content of mammalian cell membranes (12)(13)(14). Phytosomes show a bett er stability profi le than liposomes due to the unique chemical bond interact...

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Section: Merivamentioning

confidence: 99%

Curcumin phytosomal softgel formulation: Development, optimization and physicochemical characterization

Allam

Abdallah

2015

Acta Pharmaceutica

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“…Recently, gellan gum has been used as cartilage tissue surrogate materials and as an injectable, in situ forming hydrogel polymer for cellular delivery [26][27][28] . Gelatin is a highly versatile biopolymer which can be obtained at a range of isoelectric points, molecular weights and gel strengths 29 and has been used in a plethora of biomedical devices, pharmaceuticals and tissue engineering applications for over fifty years [30][31][32][33][34][35][36][37][38][39][40][41][42] . Without cross-linking, gelatin hydrogels are very weak and readily dissolve at temperatures above 29˚C which would prohibit their use in tissue engineering 43,44 .…”

Section: Introductionmentioning

confidence: 99%

Robust biopolymer based ionic–covalent entanglement hydrogels with reversible mechanical behaviour

Kirchmajer

Panhuis

2014

J. Mater. Chem. B

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Robust biopolymer based ionic-covalent entanglement hydrogels with reversible mechanical behaviour AbstractEmerging applications of hydrogels such as soft robotics and cartilage tissue scaffolds require hydrogels with enhanced mechanical performance. We report the development of a robust biopolymer based ionic-covalent entanglement network hydrogel made from calcium cross-linked gellan gum and genipin cross-linked gelatin. The ratio of the two polymers and the cross-linker concentrations significantly affected the mechanical characteristics of the hydrogels. Hydrogels with optimized composition exhibited compressive fracture stress and work of extension values of up to 1.1 ± 0.2 MPa and 230 ± 40 kJ m−3 for swelling ratios of 37.4 ± 0.6 and 19 ± 1, respectively. The compressive and tensile mechanical properties, swelling behavior (including leachage), pH sensitivity and homogeneity are discussed in detail. Fully swollen hydrogels (swelling ratio of 37.4 ± 0.6) were able to recover 95 ± 2% and 82 ± 7% of their energy dissipation (hysteresis) at 37 °C after reloading to either constant stress (150 kPa) or constant strain (50%), respectively. Emerging applications of hydrogels such as soft robotics and cartilage tissue scaffolds require hydrogels with enhanced mechanical performance. We report the development of a robust biopolymer based ionic-covalent entanglement network hydrogel made from calcium cross-linked gellan gum and genipin cross-linked gelatin. The ratio of the two polymers and the cross-linker concentrations significantly affected the mechanical characteristics of the hydrogels. Hydrogels with optimized composition exhibited compressive fracture stress and work of extension values of up to 1.1 ± 0.2 MPa and 230 ± 40 kJ.m -3 for swelling ratios of 37.4 ± 0.6 and 19 ± 1, respectively. The compressive and tensile mechanical properties, swelling behavior (including leachage), pH sensitivity and homogeneity are discussed in detail. Fully swollen hydrogels (swelling ratio of 37.4 ± 0.6) were able to recover 95 ± 2% and 82 ± 7% of their energy dissipation (hysteresis) at 37 °C after reloading to either constant stress (150 kPa) or constant strain (50%), respectively.

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“…The capsule switching test is also limited for HGCs depending on the forms of the filling materials and coating considerations. The types of materials for filling into HGCs include dry solids (e.g., powders, pellets, granules or tablets), semisolids (e.g., suspensions or pastes), and liquids (e.g., non-aqueous liquids) (48,49). The switching test can only be conducted in HGCs filled with dry solids without sealing and enteric coatings; the two pieces of an HGC shell must be separated, and the filler must be transferred out.…”

Section: Capsule Switching Testmentioning

confidence: 99%

Dissolution of Gelatin Capsules: Evidence and Confirmation of Cross-Linking

Lu¹,

Shah²

2017

Dissolution Technol.

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Cross-linking is a common problem in the dissolution of gelatin capsules. Cross-linking is characterized by a bridge across the peptide backbone of the gelatin molecule which creates water insoluble membranes or pellicles during dissolution testing. The chemical covalent bonding between gelatin chains is typically triggered by catalytic amounts of aldehyde and/or from exposure to high temperature and humidity. Cross-linking gelatin capsules results in a slower release of the drug or no release at all in common dissolution media. If the gelatin capsule dissolution fails acceptance criteria due to evidence of cross-linking, the US Pharmacopeia allows the use of enzymes in the dissolution medium and requires twotier dissolution testing. Studies have shown that drugs from cross-linked capsules are available in vivo to the patient, justifying the use of enzymes in the in vitro dissolution test. The literature contains several examples supporting evidence of cross-linking. However, confirming the degree of cross-linking continues to be a practical challenge due to a lack of quantitative procedures for measuring the extent of cross-linking and variability in options for formulations, excipients, level and types of stresses, and the experience level of the analysts. This article reviews the methodologies to confirm the evidence of cross-linking such as visual observation, capsule shell switch test, and spectroscopic determination of cross-linking, with an aim to facilitate the discussion and establishment of an acceptable standard approach.

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Soft Gelatin Capsules (Softgels)

Cited by 107 publications

References 215 publications

Curcumin phytosomal softgel formulation: Development, optimization and physicochemical characterization

Curcumin phytosomal softgel formulation: Development, optimization and physicochemical characterization

Robust biopolymer based ionic–covalent entanglement hydrogels with reversible mechanical behaviour

Dissolution of Gelatin Capsules: Evidence and Confirmation of Cross-Linking

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