scholarly journals Enhanced Water Dispersibility of Curcumin Encapsulated in Alginate-Polysorbate 80 Nano Particles and Bioavailability in Healthy Human Volunteers

2019 ◽  
Vol 7 (1) ◽  
pp. 39-56 ◽  
Author(s):  
Roopa Govindaraju ◽  
Roopa Karki ◽  
Jayanthi Chandrashekarappa ◽  
Mukunthan Santhanam ◽  
Akshay K.K. Shankar ◽  
...  
Keyword(s):  
Oral Bioavailability ◽  
Aqueous Solubility ◽  
Nano Particles ◽  
Simulated Gastric Fluid ◽  
Maximum Plasma ◽  
Polysorbate 80 ◽  
Healthy Human ◽  
Ionotropic Gelation ◽  
Quality Life ◽  
Human Volunteers

Background: The turmeric (Curcuma longa) plant, a perennial herb of the ginger family, is an agronomic crop in the south and southeast tropical Asia. Turmeric an Indian yellow gold and universal spice is described in Ayurveda, an ancient treatise on longevity and quality life for the treatment of various inflammatory disorders. The oral bioavailability of curcumin is low due to poor aqueous solubility, alkaline instability and speedy elimination. Objective: The present study is designed to prepare alginate polysorbate 80 nanoparticles to enhance aqueous solubility/dispersibility, hence bioavailability. Method: Curcumin-loaded alginate - polysorbate 80 nanoparticles were prepared by ionotropic gelation technique. Results: The optimized nano particles exhibited higher encapsulation efficiency (95%), particle size of 383 nm and Zeta potential of +200 mV. Formulations exhibited very low dissolution in Simulated Gastric Fluid (SGF) and Simulated Intestinal Fluid (SIF), but the major portion released in SCF which is attributed to the digestibility of alginate in Simulated Colonic Fluid (SCF) under the influence of colonic micro flora. FTIR and DSC observations revealed the successful entrapment of curcumin in alginate polysorbate-80 nanoparticles. The nanoparticles were more spherical, discrete and homogeneous. In healthy human volunteers, the oral bioavailability (AUC) of curcumin increased 5-fold after the consumption of curcumin nanosuspension compared to curcumin suspension. Maximum plasma concentration Cmax- 636 ± 122 ng/ml was observed at tmax- 2h for nanosuspension, whereas Cmax-87.7 ± 17.9ng/ml at tmax- 4h for suspension. Conclusion: Curcumin-loaded alginate - polysorbate 80 nanoparticles prepared by ionotropic gelation method, successfully entrapped curcumin. Both curcumin suspension and curcumin nanosuspension were safe and well tolerated and may thus be useful in the prevention or treatment of various inflammatory diseases of mankind.

Pharmacokinetics of solid lipid Boswellia serrata particles in healthy subjects

2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Preeti D. Kulkarni ◽  
Neena D. Damle ◽  
Lal Hingorani ◽  
Vaidhun H. Bhaskar ◽  
Minal R. Ghante ◽  
...  
Keyword(s):  
Plasma Concentration ◽  
Oral Bioavailability ◽  
Peak Plasma ◽  
Peak Plasma Concentration ◽  
Maximum Plasma ◽  
Boswellic Acid ◽  
Healthy Human ◽  
Boswellia Serrata ◽  
Solid Lipid ◽  
Human Volunteers

Abstract Objectives The anti-inflammatory activity of Boswellia serrata extracts (BSE) is well known. BSE comprises boswellic acids (BA) such as 3-O-acetyl-11-keto-beta-boswellic acid (AKBA) and 11-keto-boswellic acid (KBA) as major constituents. One of the limitations of BAs is their poor oral bioavailability. The aim of the study was to prepare solid lipid particles of Boswellia serrata extract (SLBSP) to enhance the bioavailability of BAs. Methods The pharmacokinetic profile of BAs was studied in 10 healthy human volunteers following a single oral dose of 333 mg of SLBSP. Pharmacokinetic blood samples were collected at 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, and 12 h post drug administration. Plasma KBA and AKBA levels were measured using a validated LC-MS/MS method. Pharmacokinetics parameters were estimated using Pheonix WinNonlin (Build 6.4.0.768) software. Results Ten healthy human volunteers were included and peak plasma concentration was achieved in 1.5 and 2.3 h for AKBA and KBA respectively. Maximum plasma concentration (C max) was 8.04 ± 1.67 ng/mL for AKBA and 23.83 ± 4.41 ng/mL for KBA whereas the corresponding area under the concentration-time curve (AUC) was 136.7 ± 56.77 ng/mL*h and 165.7 ± 24.5 ng/mL*h respectively. The elimination half-life (t 1/2) of AKBA and KBA was 6.8 ± 3.0 h and 2.45 ± 0.3 h respectively. Conclusions The SLBSP formulation of BSE showed enhanced oral bioavailability of BAs compared with historically reported data of unformulated BSE.

Pharmacokinetics of solid lipid Boswellia serrata particles in healthy subjects

2021 ◽  
Vol 36 (3) ◽  
pp. 215-221
Author(s):  
Preeti D. Kulkarni ◽  
Neena D. Damle ◽  
Lal Hingorani ◽  
Vaidhun H. Bhaskar ◽  
Minal R. Ghante ◽  
...  
Keyword(s):  
Plasma Concentration ◽  
Oral Bioavailability ◽  
Peak Plasma ◽  
Peak Plasma Concentration ◽  
Maximum Plasma ◽  
Boswellic Acid ◽  
Healthy Human ◽  
Boswellia Serrata ◽  
Solid Lipid ◽  
Human Volunteers

Abstract Objectives The anti-inflammatory activity of Boswellia serrata extracts (BSE) is well known. BSE comprises boswellic acids (BA) such as 3-O-acetyl-11-keto-beta-boswellic acid (AKBA) and 11-keto-boswellic acid (KBA) as major constituents. One of the limitations of BAs is their poor oral bioavailability. The aim of the study was to prepare solid lipid particles of Boswellia serrata extract (SLBSP) to enhance the bioavailability of BAs. Methods The pharmacokinetic profile of BAs was studied in 10 healthy human volunteers following a single oral dose of 333 mg of SLBSP. Pharmacokinetic blood samples were collected at 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, and 12 h post drug administration. Plasma KBA and AKBA levels were measured using a validated LC-MS/MS method. Pharmacokinetics parameters were estimated using Pheonix WinNonlin (Build 6.4.0.768) software. Results Ten healthy human volunteers were included and peak plasma concentration was achieved in 1.5 and 2.3 h for AKBA and KBA respectively. Maximum plasma concentration (C max) was 8.04 ± 1.67 ng/mL for AKBA and 23.83 ± 4.41 ng/mL for KBA whereas the corresponding area under the concentration-time curve (AUC) was 136.7 ± 56.77 ng/mL*h and 165.7 ± 24.5 ng/mL*h respectively. The elimination half-life (t 1/2) of AKBA and KBA was 6.8 ± 3.0 h and 2.45 ± 0.3 h respectively. Conclusions The SLBSP formulation of BSE showed enhanced oral bioavailability of BAs compared with historically reported data of unformulated BSE.

scholarly journals Manufacturing Different Types of Solid Dispersions of BCS Class IV Polyphenol (Daidzein) by Spray Drying: Formulation and Bioavailability

Pharmaceutics ◽  
2019 ◽  
Vol 11 (10) ◽  
pp. 492 ◽  
Author(s):  
Gean Pier Panizzon ◽  
Fernanda Giacomini Bueno ◽  
Tânia Ueda-Nakamura ◽  
Celso Vataru Nakamura ◽  
Benedito Prado Dias Filho
Keyword(s):  
Plasma Concentration ◽  
Spray Drying ◽  
Oral Bioavailability ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
Maximum Plasma ◽  
Third Generation ◽  
Different Types ◽  
Class Iv

Daidzein (DZ) is a polyphenolic compound belonging to Biopharmaceutical Classification System class IV, which shows that it may have limited therapeutic effects due to its low solubility and poor bioavailability. This study aimed to obtain high-purity DZ and prepare and characterize different types of solid dispersions (SDs) in order to enhance aqueous solubility and bioavailability. Excipients were investigated in order to manufacture different types of solid dispersions (SDs). Second-generation solid dispersions (SG), third-generation solid dispersions (TG), and second- and third-generation pH-modulated solid dispersions (SD and TG pHM-SD) were produced via spray drying. The SDs were characterized and tested for in vitro DZ release and oral bioavailability. SDs have shown increased aqueous solubility and in vitro release rate. Solid-state characterization showed that DZ was in an amorphous state in most of the formulations. The enhanced aqueous solubility of TG-pHM SD was reflected by an increase in oral bioavailability, which significantly increased the maximum plasma concentration approximately 20-fold and decreased the time to reach the maximum plasma concentration. The production of pHM SDs that contain DZ via spray drying is a simple and effective approach for oral drug delivery, which has the potential to greatly reduce the dose and enhance therapeutics effects.

Effect of silymarin pretreatment on the bioavailability of domperidone in healthy human volunteers

2014 ◽  
Vol 29 (4) ◽  
Author(s):  
Shravan Kumar Yamsani ◽  
Madhusudan Rao Yamsani
Keyword(s):  
Oral Bioavailability ◽  
Pharmacokinetic Parameters ◽  
Rat Intestine ◽  
Healthy Human ◽  
P Glycoprotein ◽  
Human Volunteers ◽  
Significant Difference

AbstractThe aim of this study was to investigate the effect of silymarin pretreatment on domperidone oral bioavailability in humans.The rats were pretreated with silymarin for 7 days. The transport of domperidone across the rat intestine (duodenum, jejunum, ileum, and colon) was studied by usingIn the everted sac and non-everted sac study with silymarin pretreatment, domperidone transport increased from the duodenum, jejunum, ileum, and colon. The silymarin pretreatment increased the bioavailability of domperidone. There was a statistically significant difference in the pharmacokinetic parameters CThe significant difference in absorption of domperidone on pretreatment with silymarin is due to the inhibition of P-glycoprotein and CYP3A. Silymarin, which inhibits CYP3A4, should be contraindicated for domperidone.

EFFECT OF SILYMARIN ON THE ORAL BIOAVAILABILITY OF RANITIDINE IN HEALTHY HUMAN VOLUNTEERS

2007 ◽  
Vol 22 (2-3) ◽  
Author(s):  
B. Nageshwar Rao ◽  
Maddi Srinivas ◽  
Y. Shravan Kumar ◽  
Y. Madhusudan Rao
Keyword(s):  
Oral Bioavailability ◽  
Healthy Human ◽  
Human Volunteers

scholarly journals Investigating the Potential of Transmucosal Delivery of Febuxostat from Oral Lyophilized Tablets Loaded with a Self-Nanoemulsifying Delivery System

Pharmaceutics ◽  
2020 ◽  
Vol 12 (6) ◽  
pp. 534 ◽  
Author(s):  
Yasir A. Al-Amodi ◽  
Khaled M Hosny ◽  
Waleed S. Alharbi ◽  
Martin K. Safo ◽  
Khalid M El-Say
Keyword(s):  
Oral Bioavailability ◽  
Area Under The Curve ◽  
Stability Index ◽  
The United States ◽  
Maximum Plasma ◽  
Large Area ◽  
Healthy Human ◽  
Disintegration Time ◽  
Maximum Stability ◽  
Transmucosal Delivery

Gout is the most familiar inflammatory arthritis condition caused by the elevation of uric acid in the bloodstream. Febuxostat (FBX) is the latest drug approved by the United States Food and Drug Administration (US FDA) for the treatment of gout and hyperuricemia. FBX is characterized by low solubility resulting in poor gastrointestinal bioavailability. This study aimed at improving the oral bioavailability of FBX by its incorporation into self-nanoemulsifying delivery systems (SNEDS) with minimum globule size and maximum stability index. The SNEDS-incorporated FBX was loaded into a carrier substrate with a large surface area and lyophilized with other excipients to produce a fluffy, porous-like structure tablet for the transmucosal delivery of FBX. The solubility of FBX was studied in various oils, surfactants, and cosurfactants. Extreme vertices design was utilized to optimize FBX-SNEDS, and subsequently loaded into lyophilized tablets along with suitable excipients. The percentages of the main tablet excipients were optimized using a Box–Behnken design to develop self-nanoemulsifying lyophilized tablets (SNELTs) with minimum disintegration time and maximum drug release. The pharmacokinetics parameters of the optimized FBX-SNELTs were tested in healthy human volunteers in comparison with the marketed FBX tablets. The results revealed that the optimized FBX-SNELTs increased the maximum plasma concentration (Cmax) and decreased the time to reach Cmax (Tmax) with a large area under the curve (AUC) as a result of the enhanced relative oral bioavailability of 146.4%. The significant enhancement of FBX bioavailability is expected to lead to reduced side effects and frequency of administration during the treatment of gout.

Enhanced Oral Bioavailability of Ibrutinib Encapsulated Poly (Lactic-co- Glycolic Acid) Nanoparticles: Pharmacokinetic Evaluation in Rats

2019 ◽  
Vol 15 (6) ◽  
pp. 661-668 ◽  
Author(s):  
Abdullah S. Alshetaili ◽  
Mohammad J. Ansari ◽  
Md. K. Anwer ◽  
Majid A. Ganaie ◽  
Muzaffar Iqbal ◽  
...  
Keyword(s):  
Oral Bioavailability ◽  
Compartmental Analysis ◽  
Aqueous Solubility ◽  
Plga Nanoparticles ◽  
Albino Rats ◽  
Maximum Plasma ◽  
Nanoprecipitation Method ◽  
Poorly Soluble ◽  
Development Phases ◽  
Wistar Albino Rats

Background: The poor oral bioavailability of newly discovered chemical entities and marketed formulations are usually related to poor aqueous solubility or poor permeability, leading to drug failure in the development phases or therapeutic failure in a clinical setting. However, advancement in drug formulations and delivery technologies have enabled scientists to improve the bioavailability of formulations by enhancing solubility or permeability. Objective: This study reports the enhancement of the oral bioavailability of ibrutinib (IBR), a poorly soluble anticancer drug in Wistar albino rats. Methods: IBR loaded nanoparticles were formulated through the nanoprecipitation method by utilizing poly lactide-co-glycolide (PLGA) as a safe, biodegradable and biocompatible polymer, and poloxamer or pluronic 127 as a stabilizer. Animals were administered with a dose of 10 mg/kg of IBR suspension or an equivalent amount of IBR loaded nanoparticles. Plasma samples were extracted and analyzed by state of the art UPLC-MS/MS technique. Pharmacokinetic (PK) parameters and bioavailability were calculated by non-compartmental analysis. Results: There was an approximately 4.2-fold enhancement in the oral bioavailability of IBR-loaded nanoparticles, as compared to the pure IBR suspension. The maximum plasma concentration (Cmax; 574.31 ± 56.20 Vs 146.34 ± 5.37 ng/mL) and exposure (AUC; 2291.65 ± 263.83 vs 544.75 ± 48.33 ng* h/mL) of IBR loaded nanoparticles were significantly higher than those exhibited through pure IBR suspension. Conclusion: The outcomes of the present study suggested the potential of PLGA nanoparticles in the enhancement of bioavailability and the therapeutic efficacy of IBR.

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