Pharmacosomes: the lipid-based new drug delivery system

Semalty, Ajay; Semalty, Mona; Rawat, Balwant; Singh, Devendra; Rawat, Mahiraj Singh

doi:10.1517/17425240902967607

Cited by 138 publications

(57 citation statements)

References 30 publications

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“…Broadly, vesicular carriers are divided into two main classes: liposomes, which represent the groundbreaking discovery of Alec Bangham in the 1960s and are composed mainly of phosphatidylcholine (PC) and cholesterol (CH) bilayers, and niosomes that were revealed later in 1970, by L'Oreal, and denote non-ionic surfactant vesicles (Torchilin, 2005). Following that, newer forms of lipid vesicles were presented by various researchers and includes tranferosomes (Bragagni et al, 2012), emulsomes (Vyas et al, 2006), enzymosomes (Gaspar et al, 2003), ethosomes (Pandey et al, 2014) and pharmacosomes (Semalty et al, 2009).…”

Section: Vesicular Carriersmentioning

confidence: 99%

Bile salts-containing vesicles: promising pharmaceutical carriers for oral delivery of poorly water-soluble drugs and peptide/protein-based therapeutics or vaccines

Aburahma¹

2014

Drug Delivery

103

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Most of the new drugs, biological therapeutics (proteins/peptides) and vaccines have poor performance after oral administration due to poor solubility or degradation in the gastrointestinal tract (GIT). Though, vesicular carriers exemplified by liposomes or niosomes can protect the entrapped agent to a certain extent from degradation. Nevertheless, the harsh GIT environment exemplified by low pH, presence of bile salts and enzymes limits their capabilities by destabilizing them. In response to that, more resistant bile salts-containing vesicles (BS-vesicles) were developed by inclusion of bile salts into lipid bilayers constructs. The effectiveness of orally administrated BS-vesicles in improving the performance of vesicles has been demonstrated in researches. Yet, these attempts did not gain considerable attention. This is the first review that provides a comprehensive overview of utilizing BS-vesicles as a promising pharmaceutical carrier with a special focus on their successful applications in oral delivery of therapeutic macromolecules and vaccines. Insights on the possible mechanisms by which BSvesicles improve the oral bioavailability of the encapsulated drug or immunological response of entrapped vaccine are explained. In addition, methods adopted to prepare and characterize BSvesicles are described. Finally, the gap in the scientific researches tackling BS-vesicles that needs to be addressed is highlighted.

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Section: Vesicular Carriersmentioning

confidence: 99%

Bile salts-containing vesicles: promising pharmaceutical carriers for oral delivery of poorly water-soluble drugs and peptide/protein-based therapeutics or vaccines

Aburahma¹

2014

Drug Delivery

103

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“…6,10 Liposomal formulations are adjustable to improve drug solubility and stability, enhance their bioavailability, modify tissue distribution profiles of drugs, and target specific organs in cancer or inflammatory diseases. [11][12][13] Takahama et al 6 investigated the effects of liposomal amiodarone on lethal arrhythmias and hemodynamic parameters in an ischemia/reperfusion rat model. They discovered that the liposomal amiodarone targeting ischemic/reperfused myocardium could reduce the mortality due to lethal arrhythmia and the negative hemodynamic changes caused by amiodarone.…”

Section: Introductionmentioning

confidence: 99%

Preparation of liposomal amiodarone and investigation of its cardiomyocyte-targeting ability in cardiac radiofrequency ablation rat model

Zhuge¹,

Zheng²,

Xie³

et al. 2016

IJN

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The objective of this study was to develop an amiodarone hydrochloride (ADHC)-loaded liposome (ADHC-L) formulation and investigate its potential for cardiomyocyte targeting after cardiac radiofrequency ablation (CA) in vivo. The ADHC-L was prepared by thin-film method combined with ultrasonication and extrusion. The preparation process was optimized by Box–Behnken design with encapsulation efficiency as the main evaluation index. The optimum formulation was quantitatively obtained with a diameter of 99.9±0.4 nm, a zeta potential of 35.1±10.9 mV, and an encapsulation efficiency of 99.5%±13.3%. Transmission electron microscopy showed that the liposomes were spherical particles with integrated bilayers and well dispersed with high colloidal stability. Pharmacokinetic studies were investigated in rats after intravenous administration, which revealed that compared with free ADHC treatment, ADHC-L treatment showed a 5.1-fold increase in the area under the plasma drug concentration–time curve over a period of 24 hours (AUC 0–24 h ) and an 8.5-fold increase in mean residence time, suggesting that ADHC-L could facilitate drug release in a more stable and sustained manner while increasing the circulation time of ADHC, especially in the blood. Biodistribution studies of ADHC-L demonstrated that ADHC concentration in the heart was 4.1 times higher after ADHC-L treatment in CA rat model compared with ADHC-L sham-operated treatment at 20 minutes postinjection. Fluorescence imaging studies further proved that the heart-targeting ability of ADHC-L was mainly due to the CA in rats. These results strongly support that ADHC-L could be exploited as a potential heart-targeting drug delivery system with enhanced bioavailability and reduced side effects for arrhythmia treatment after CA.

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“…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 interaction between phospholipid molecules and polyphenolic compounds (15).…”

Section: Introductionmentioning

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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Pharmacosomes: the lipid-based new drug delivery system

Cited by 138 publications

References 30 publications

Bile salts-containing vesicles: promising pharmaceutical carriers for oral delivery of poorly water-soluble drugs and peptide/protein-based therapeutics or vaccines

Bile salts-containing vesicles: promising pharmaceutical carriers for oral delivery of poorly water-soluble drugs and peptide/protein-based therapeutics or vaccines

Preparation of liposomal amiodarone and investigation of its cardiomyocyte-targeting ability in cardiac radiofrequency ablation rat model

Curcumin phytosomal softgel formulation: Development, optimization and physicochemical characterization

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