Recent advances and future prospects of phyto-phospholipid complexation technique for improving pharmacokinetic profile of plant actives

Khan, Junaid; Alexander, Amit; AJAZUDDIN, .; Saraf, Shailendra

doi:10.1016/j.jconrel.2013.02.025

Cited by 215 publications

(101 citation statements)

References 58 publications

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“…Incorporating bioactive phytoconstituents into phospholipid molecules is reported to improve the aqueous solubility, the membrane permeability, and hence the systemic absorption and bioavailability of the active phytoconstituents. Such complexes are appropriately called phytosomes, herbosomes, or naturosomes (3,4). Studies have reported success in improving the pharmacological profiles of several bioactive phytoconstituents using drugphospholipid complexation technique (5-9).…”

Section: Introductionmentioning

confidence: 99%

Preparation and Evaluation of Phospholipid-Based Complex of Standardized Centella Extract (SCE) for the Enhanced Delivery of Phytoconstituents

Saoji

Raut

Dhore

et al. 2015

AAPS J

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Abstract. In the present study, a phospholipid-based complex of standardized Centella extract (SCE) was developed with a goal of improving the bioavailability of its phytoconstituents. The SCE-phospholipid complex was prepared by solvent evaporation method and characterized for its physicochemical and functional properties. Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), scanning electron microscopy (SEM), photomicroscopy, and powder x-ray diffraction (PXRD) were used to confirm the formation of Centella naturosome (CN). The prepared complex was functionally evaluated by apparent solubility, in vitro drug release, ex vivo permeation, and in vivo efficacy studies. The prepared CN exhibited a significantly higher (12-fold) aqueous solubility (98.0±1.4 μg/mL), compared to the pure SCE (8.12±0.44 μg/mL), or the physical mixture of SCE and the phospholipid (13.6±0.4 μg/mL). The in vitro dissolution studies revealed a significantly higher efficiency of CN in releasing the SCE (99.2±4.7, % w/w) in comparison to the pure SCE (39.2±2.3, % w/w), or the physical mixture (42.8±2.09, % w/w). The ex vivo permeation studies with the everted intestine method showed that the prepared CN significantly improved the permeation of SCE (82.8±3.7, % w/w), compared to the pure SCE (26.8±2.4, % w/w), or the physical mixture (33.0±2.7, % w/w). The in vivo efficacy studies using the Morris Water Maze test indicated a significant improvement of the spatial learning and memory in aged mice treated with CN. Thus, drug-phospholipid complexation appears to be a promising strategy to improve the aqueous solubility and bioavailability of bioactive phytoconstituents.

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Section: Introductionmentioning

confidence: 99%

Preparation and Evaluation of Phospholipid-Based Complex of Standardized Centella Extract (SCE) for the Enhanced Delivery of Phytoconstituents

Saoji

Raut

Dhore

et al. 2015

AAPS J

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“…The entrapment efficiency was calculated according to the following formula: [15][16] Entrapment efficiency (%) = (Total amount of drug) -(Amount of free drug) / (Total amount of drug) × 100…”

Section: Drug Entrapment Efficiencymentioning

confidence: 99%

Formulation and Evaluation of Capsules of Syzygium Cumini Phytosomes

Amudha¹,

Manna²,

Jeganathan³

2018

J. Pharm. Sci. Innov.

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The objective of the study was to develop a novel Phytosome formulation of Syzygium cumini capsules by incorporation of phospholipids, for the improved permeability, solubility and better physical characteristics. The Syzygium cumini phytosome capsules were prepared by using Thin Film Hydration Technique method and were optimized. The formations of phytosomes were analyzed for microscopic view, SEM, TEM, measurement of particle size & zeta potential, drug entrapment efficiency, drug content, In vitro dissolution studies and also the release kinetics of Syzygium cumini phytosomes complex. The Syzygium cumini phytosome capsules prepared by using Thin Film Hydration Technique showed a good microscopic view and practical yield, the drug content, SEM, TEM, measurement of particle size & zeta potential and other in vitro studies were resulted as anticipated. The Syzygium cumini phytosome capsules were found to show better solubility and compatibility with the excipients, it is concluded that Syzygium cumini extract phytosomes has better physical characteristics and improved permeability, solubility than that of extract to overcome ability to cross lipid-rich biological membranes and which results in increase oral bioavailability.

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“…Hasil tersebut menunjukkan bahwa rata-rata diameter partikel nano-fitosom yang dibuat sesuai dengan ukuran rata-rata diameter partikel hasil kompleksasi antara bahan aktif pada tanaman dengan fosfatidilkolin berada pada rentang 50 nm -500 µm. 15 Berdasarkan hasil evaluasi ukuran dan distribusi ukuran partikel, nanofitosom yang dibuat telah memenuhi kriteria inklusi yang ditetapkan yaitu ukuran partikel ≤ 200 nm dengan indeks polidispersitas 0-0,5. Oleh karena itu, dapat dilakukan evaluasi efisiensi penjerapan terhadap nano-fitosom yang telah dibuat.…”

Section: Tabelunclassified

Pengembangan Formula Nano-fitosom Serbuk Liofilisasi Seduhan Teh Hitam (Camellia sinensis L. Kuntze)

Husni

Puspitaningrum

2017

IJPST

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AbstrakNano-fitosom merupakan suatu teknologi nano yang digunakan untuk meningkatkan bioavailabilitas bahan aktif yang terkandung dalam tanaman dengan cara mengikat bahan aktif dengan fosfolipid yang memiliki sifat mirip dengan membran sel. Nano-fitosom dibuat dengan mencampurkan fitokonstituen dan fosfatidilkolin dalam perbandingan molar tertentu. Penelitian ini bertujuan untuk mengembangkan formula nano-fitosom serbuk liofilisasi seduhan teh hitam (Camellia sinensis L. Kuntze). Nano-fitosom diformulasikan dengan membuat tiga variasi perbandingan katekin:fosfatidilkolin:kolesterol mulai dari 1:1:0,2 (F1), 1:2:0,2 (F2), dan 1:3:0,2 (F3) dengan menggunakan metode refluks. Evaluasi nano-fitosom meliputi ukuran partikel, indeks polidispersitas, dan efisiensi penjerapan. Hasil evaluasi menunjukkan bahwa ukuran partikel nano-fitosom sekitar 52,1-101,9 nm dengan nilai indeks polidispersitas 0,309-0,404. Efisiensi penjerapan berkisar antara 6,7266%-11,4317%. Formula nano-fitosom dengan efisiensi penjerapan yang paling baik yaitu F 3 dengan perbandingan molar katekin:fosfatidilkolin:kolesterol 1:3:0,2 dengan ukuran partikel sebesar 52,1±12,5 nm, indeks polidispersitas 0,320 dan efisiensi penjerapan 11,4317±0,3153%. Analisis data menggunakan One-Way Anova menunjukkan bahwa terdapat pengaruh konsentrasi fosfatidilkolin terhadap efisiensi penjerapan secara signifikan (p < 0,05).Kata kunci: nano-fitosom, fosfatidilkolin, teh hitam, Camellia sinensis L. Kuntze Development of Nano-phytosome Formula of Brewed Black Tea (Camellia sinensis L. Kuntze) Lyophilization PowderAbstract Nano-phytosome is a nanotechnology for increasing the bioavailability of active ingredient in the plant by binding the active ingredient with a phospholipid which has properties similiar to cell membrane. Nano-phytosome was made by mixing the phytoconstituent and phosphatidylcholine in particular molar ratio. The aim of this study was to develop nanophytosome formula of brewed black tea (Camellia sinensis L. Kuntze) lyophilization powder. Nano-phytosome was formulated in three variations of molar ratio of phytoconstituent:phosphatidylcholine:cholesterol (1:1:0.2 (F 1 ), 1:2:0.2 (F 2 ) and 1:3:0.2 (F 3 )) using reflux method. Evaluation of the nano-phytosome include particle size, polydispersity index, and entrapment efficiency. The study results showed that the particle size of nanophytosome was 52.1-101.9 nm with polydispersity index 0.309-0.404. Entrapment efficiency was approximately between 6.7266%-11.4317%. The best entrapment efficiency of the nanophytosome formula was F3 which molar ratio of catechin: phosphatidylcholine: cholesterol 1:3:0.2 with 52.1±12.5 nm in diameter, 0.302 in polydispersity index and 11,4317±0,3153% in entrapment efficiency. Analysis data using One-Way Anova showed that the concentration of phosphatidylcholine influenced the entrapment efficiency significantly (p < 0.05).

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Recent advances and future prospects of phyto-phospholipid complexation technique for improving pharmacokinetic profile of plant actives

Cited by 215 publications

References 58 publications

Preparation and Evaluation of Phospholipid-Based Complex of Standardized Centella Extract (SCE) for the Enhanced Delivery of Phytoconstituents

Preparation and Evaluation of Phospholipid-Based Complex of Standardized Centella Extract (SCE) for the Enhanced Delivery of Phytoconstituents

Formulation and Evaluation of Capsules of Syzygium Cumini Phytosomes

Pengembangan Formula Nano-fitosom Serbuk Liofilisasi Seduhan Teh Hitam (Camellia sinensis L. Kuntze)

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