Enhancement of bioavailability through transdermal drug delivery of paliperidone palmitate-loaded nanostructured lipid carriers

2021 ◽  
Author(s):  
Shilpa Raval ◽  
Parva Jani ◽  
Pravin Patil ◽  
Parth Thakkar ◽  
Krutika Sawant
Keyword(s):  
Drug Delivery ◽  
Oral Drug Delivery ◽  
Ex Vivo ◽  
Drug Loading ◽  
Physicochemical Characterization ◽  
Nanostructured Lipid Carriers ◽  
Paliperidone Palmitate ◽  
Oral Drug ◽  
Pharmacokinetic Studies ◽  
Transdermal Patch

Aim: The work describes enhanced bioavailability of paliperidone palmitate through transdermal delivery using nanostructured lipid carriers (NLC). Materials & methods: NLCs were formulated by nanoprecipitation method followed by incorporation in transdermal patch and physicochemical characterization. Results: NLCs showed high percentage entrapment efficiency of 83.44 ± 0.8%, drug loading of 24.75 ± 1.10% (w/w), particle size of 173.8 ± 3.25 nm, polydispersity index of 0.143 ± 0.05 and zeta potential of -15.9 ± 0.75 mV. In vitro and ex vivo studies indicated zero-order controlled drug release from NLCs and transdermal patch up to 48 h. Pharmacokinetic studies indicated 1.76-fold enhanced bioavailability by transdermal route as compared with oral drug delivery. Conclusion: From the results, it was concluded that drug-loaded NLCs-transdermal patch is promising drug delivery system for poorly bioavailable drugs.

scholarly journals SPRAY DRIED LACTOSE BASED PRONIOSOMES AS STABLE PROVESICULAR DRUG DELIVERY CARRIERS: SCREENING, FORMULATION, AND PHYSICOCHEMICAL CHARACTERIZATION

2018 ◽  
Vol 10 (5) ◽  
pp. 125 ◽  
Author(s):  
Ali Nasr ◽  
Mona Qushawy ◽  
Shady Swidan
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Zeta Potential ◽  
Oral Drug Delivery ◽  
Physicochemical Characterization ◽  
Water Soluble ◽  
Oral Drug ◽  
Flow Properties ◽  
Poorly Water Soluble ◽  
Spray Dried

Objective: In the present investigation efforts were considered to optimize the different conditions for the preparation of spray dried lactose based proniosomes. The aim of this research was to investigate the feasibility of proniosomes as stable precursors for the development of niosomes as oral drug delivery system for poorly water-soluble drugs.Methods: A total of twenty-eight plain proniosomal formulae were prepared with various surfactant-cholesterol loading ratios in each formula using spray dried lactose as a carrier. Span 20, 40, 60 and 80 were used in various molar ratios with cholesterol. Different evaluation techniques were performed to study the performance of the prepared proniosomes. The micromeritic properties of the prepared proniosomes were analyzed. The reconstituted niosomes were further evaluated for morphological characterization using transmission electron microscope (TEM), particle size analysis, zeta potential, and polydispersity index (PDI). Finally, selected proniosomal formulae were tested for stability study.Results: The proniosomal formulae prepared using span 40 and span 60 exhibited excellent flowability while those prepared with span 20 and span 80 showed poor flow properties. TEM photographs revealed that the vesicles were discrete, spherical without aggregation. The mean vesicle size of reconstituted niosomes was found to be in the range between (252.9±0.43–624.3±0.23 nm) with perfect PDI values (0.387±0.05–0.835±0.03). The negative values of zeta potential indicated that all prepared formulae were stabilized by electrostatic repulsion forces. Stability studies confirmed that proniosomes give a more stable system that could overcome the problems of standard niosomes. Formulae with the smallest particle size, higher surface charge values and best flow properties were selected to be loaded with poorly soluble drugs for further study.Conclusion: The obtained results offered evidence that spray-dried lactose based proniosomes are promising stable drug delivery carriers and ready to incorporate various poorly water-soluble drugs in order to improve their limited oral bioavailability.

scholarly journals Rapid Synthesis of Superabsorbent Smart-Swelling Bacterial Cellulose/Acrylamide-Based Hydrogels for Drug Delivery

2013 ◽  
Vol 2013 ◽  
pp. 1-10 ◽  
Author(s):  
Manisha Pandey ◽  
Mohd Cairul Iqbal Mohd Amin ◽  
Naveed Ahmad ◽  
Muhammad Mustafa Abeer
Keyword(s):  
Drug Delivery ◽  
Bacterial Cellulose ◽  
Oral Drug Delivery ◽  
Drug Loading ◽  
Solvent System ◽  
Physicochemical Characteristics ◽  
Oral Drug ◽  
X Ray Diffraction ◽  
Spectroscopy Analysis ◽  
Drug Release Profile

This study evaluated the effect of solubilized and dispersed bacterial cellulose (BC) on the physicochemical characteristics and drug release profile of hydrogels synthesized using biopolymers. Superabsorbent hydrogels were synthesized by graft polymerization of acrylamide on BC solubilized in an NaOH/urea solvent system and on dispersed BC by usingN,N′-methylenebisacrylamide as a crosslinker under microwave irradiation. Fourier transform infrared spectroscopy analysis of the resulting hydrogels confirmed the grafting, and an X-ray diffraction pattern showed a decrease in the crystallinity of BC after the grafting process. The hydrogels exhibited pH and ionic responsive swelling behavior, with hydrogels prepared using solubilized BC (SH) having higher swelling ratios. Furthermore, compared to the hydrogels synthesized using dispersed BC, the hydrogels synthesized using solubilized BC showed higher porosity, drug loading efficiency, and release. These results suggest the superiority of the hydrogels prepared using solubilized BC and that they should be explored further for oral drug delivery.

Microencapsulation of nanoparticles with enhanced drug loading for pH-sensitive oral drug delivery for the treatment of colon cancer

2012 ◽  
Vol 129 (2) ◽  
pp. 714-720 ◽  
Author(s):  
Yichao Wang ◽  
Puwang Li ◽  
Zheng Peng ◽  
Feng Hua She ◽  
Ling Xue Kong
Keyword(s):  
Drug Delivery ◽  
Colon Cancer ◽  
Oral Drug Delivery ◽  
Drug Loading ◽  
Ph Sensitive ◽  
Oral Drug

scholarly journals Development of Polymeric Nanoparticles ofGarcinia mangostanaXanthones in Eudragit RL100/RS100 for Anti-Colon Cancer Drug Delivery

2015 ◽  
Vol 2015 ◽  
pp. 1-12 ◽  
Author(s):  
Abdalrahim F. A. Aisha ◽  
Amin Malik Shah Abdulmajid ◽  
Zhari Ismail ◽  
Salman A. Alrokayan ◽  
Khalid M. Abu-Salah
Keyword(s):  
Electron Microscopy ◽  
Drug Delivery ◽  
Colon Cancer ◽  
Oral Drug Delivery ◽  
Polymeric Nanoparticles ◽  
Drug Loading ◽  
Intracellular Delivery ◽  
Oral Drug ◽  
Cancer Drug ◽  
Freeze Dried

Xanthones are a group of oxygenated heterocyclic compounds with anticancer properties, but poor aqueous solubility and low oral bioavailability hinder their therapeutic application. This study sought to prepare a xanthones extract (81%  α-mangostin and 16%  γ-mangostin) in polymeric nanoparticles and to investigate its intracellular delivery and cytotoxicity toward colon cancer cells. The nanoparticles were prepared in Eudragit RL100 and Eudragit RS100 by the nanoprecipitation method at drug loading and entrapment efficiency of 20% and >95%, respectively. Freeze-drying of bulk nanoparticle solutions, using glucose or sucrose as cryoprotectants, allowed the collection of nanoparticles at >95% yield. Solubility of the xanthones extract was improved from 0.1 µg/mL to 1250 µg/mL. Transmission electron microscopy (TEM) and dynamic light scattering (DLS) of the freeze-dried final formulation showed the presence of cationic round nanoparticles, with particle size in the range of 32–130 nm. Scanning electron microscopy (SEM) showed the presence of nanospheres, and Fourier transform infrared (FTIR) spectroscopy indicated intermolecular interaction of xanthones with Eudragit polymers. Cellular uptake of nanoparticles was mediated via endocytosis and indicated intracellular delivery of xanthones associated with potent cytotoxicity (median inhibitory concentration26.3±0.22 µg/mL). Presented results suggest that cationic nanoparticles of xanthones may provide a novel oral drug delivery system for chemoprevention or treatment of intestinal and colon tumors.

Effects of surface hydrophilic properties of PEG-based mucus-penetrating nanostructured lipid carriers on oral drug delivery

RSC Advances ◽  
2016 ◽  
Vol 6 (87) ◽  
pp. 84164-84176 ◽  
Author(s):  
Huipeng Li ◽  
Nida El Islem Guissi ◽  
Zhigui Su ◽  
Qineng Ping ◽  
Minjie Sun
Keyword(s):  
Drug Delivery ◽  
Oral Drug Delivery ◽  
Structured Lipid ◽  
Nanostructured Lipid Carriers ◽  
Oral Drug

Nano-structured lipid carriers (NLCs) can be changed into nanostructured lipid carriers (NLCs).

scholarly journals Permeation enhancement effects of leaf materials from different aloe species on in vitro and ex vivo nasal epithelial models

2020 ◽  
Vol 9 (4) ◽  
pp. 355-365
Author(s):  
Werner Gerber ◽  
Dewald Steyn ◽  
Awie Kotzé ◽  
Hanna Svitina ◽  
Ché Weldon ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Oral Drug Delivery ◽  
Cell Model ◽  
Ex Vivo ◽  
Aloe Vera ◽  
Neutral Red ◽  
Oral Drug ◽  
Nasal Drug Delivery ◽  
Aloe Ferox

Introduction: The nasal route of drug administration offers an alternative way for oral drug delivery and has the benefit of avoiding first-pass metabolism through drug delivery directly into the systemic circulation. The drug absorption enhancing effects of selected aloe leaf materials have been shown across various delivery routes, but their efficacies in this regard across nasal epithelia have not yet been investigated. The aim of this study was to determine the effects of gel and whole leaf extract materials from three selected aloe species (Aloe vera, Aloe ferox and Aloe muth-muth) on FITC-dextran 4400 permeation across two nasal epithelial models. Methods: Permeation of FITC-dextran 4400 and histological studies were conducted on both RPMI 2650 cell layers and excised sheep nasal mucosa, while toxicity studies were conducted using a neutral red assay on the RPMI 2650 cell model. Results: Significantly increased (P ≤ 0.05) apparent permeability coefficient (Papp) values of FITC-dextran 4400 in the presence of the aloe materials as compared to the control were found with all three aloe species at the highest concentrations (1.5% and 3% w/v) in the RPMI 2650 cell line, while only Aloe muth-muth at the highest concentration exhibited significantly (P ≤ 0.05) higher Papp values across the excised tissue model. Histological and neutral red analysis showed that Aloe vera materials exhibited detrimental effects, Aloe muth-muth only showed slight effects on cell viability and Aloe ferox exhibited no effect on the nasal epithelium. Conclusion: This in vitro study showed for the first time the potential of Aloe ferox and Aloe muth-muth leaf materials to enhance nasal drug delivery without causing damaging effects on the epithelium, while Aloe vera enhanced nasal drug delivery with detrimental effects as determined by means of cytotoxicity assays and histological analysis.

Construction and evaluation of liraglutide delivery system based on milk exosomes: a new idea for oral peptide delivery

2021 ◽  
Vol 22 ◽  
Author(s):  
Yanan Shi ◽  
Shiqi Guo ◽  
Yanzi Liang ◽  
Lanze Liu ◽  
Aiping Wang ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Oral Drug Delivery ◽  
Drug Loading ◽  
Oral Drug ◽  
Freeze Thaw ◽  
Loading Methods ◽  
Incubation Method ◽  
Oral Drug Delivery Systems ◽  
Extrusion Method

Background: Increasing the bioavailability of peptide or protein drugs has always been an essential topic in pharmacy. Milk exosomes as a carrier for oral drug delivery systems have begun to attract attention in recent years. The application of oral milk exosomes carriers to peptide drugs such as liraglutide is worth trying. Objective: Milk-derived exosomes are used in this study to encapsulate the GLP-1 receptor agonist liraglutide. It also explored the feasibility of using this drug delivery system for oral biomolecules delivery in the future. Methods: The size and morphology of milk exosomes were characterized. The gastrointestinal stability of milk exosomes was evaluated in a dialysis bag. The cellular uptake of milk exosomes in an intestinal cell was observed. Six drug loading methods have been evaluated and compared preliminarily, and they are the incubation method, sonication method, extrusion method, freeze-thaw cycles method, saponin-assisted method, and electroporation method. Results: As demonstrated in this study, milk exosomes showed significant stability in the gastrointestinal environment and excellent affinity with intestinal cells, indicating their unique benefits used for oral drug delivery. Effective drug loading method for exosomes is challenging. Among the six drug loading methods used in this study, the liraglutide-Exo prepared by the extrusion method obtained the most significant drug load, which was 2.45 times the direct incubation method. The liraglutide-Exo obtained by the freeze-thaw cycles method has the slightest morphological change. Conclusion: The study showed milk exosome-based oral drug delivery systems are promising.

Size-exclusive effect of nanostructured lipid carriers on oral drug delivery

2016 ◽  
Vol 511 (1) ◽  
pp. 524-537 ◽  
Author(s):  
Huipeng Li ◽  
Minglei Chen ◽  
Zhigui Su ◽  
Minjie Sun ◽  
Qineng Ping
Keyword(s):  
Drug Delivery ◽  
Oral Drug Delivery ◽  
Nanostructured Lipid Carriers ◽  
Oral Drug

scholarly journals Synthesis and Characterization of Starch-Graft-Acrylamide Hydrogel for Oral Drug Delivery

2020 ◽  
Vol 27 (2) ◽  
pp. 16-21
Author(s):  
H. Musa ◽  
Y. Musa ◽  
M. Suleiman
Keyword(s):  
Drug Delivery ◽  
Oral Drug Delivery ◽  
Drug Loading ◽  
Oral Drug ◽  
Intestinal Fluid ◽  
Simulated Intestinal Fluid ◽  
Swelling Capacity ◽  
Model Drug ◽  
Polymerization Method

In this research, starch was extracted from fresh sweet potato and was used to prepare starch-g-acrylamide hydrogel using free radical polymerization method with potassium per sulphate and N’N-Methylene bisacrylamide as initiator and cross-linker, respectively. The swelling capacity and pH sensitivity of the synthesized hydrogel were investigated in solutions of various pH (1-12). The drug loading and release experiment was also carried out using promethazine (PMZ) as the model drug at 25oC and 37oC, respectively while the release study was carried out in an enzyme-free simulated gastric intestinal fluid (SGF) and simulated intestinal fluid (SIF). The result showed a 905% swelling at pH 11, suggesting increased swelling capacity at higher pH values. Drug loading result indicated 99% of the drug was entrapped by the hydrogel as confirmed by UV-visible spectrophotometry. SIF and SGF Simulation indicated a 24% and 9% drug release for the first ten hours. At the end of 48 hours the release was 96% and 89%, respectively indicating the hydrogel released more promethazine in SIF than in SGF. The results obtained in this work suggest that starch-graft-acrylamide hydrogel is a potential vehicle for oral drug delivery. Keywords: Starch, Acrylamide, Hydrogel, Drug delivery.

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