scholarly journals Folate and Borneol Modified Bifunctional Nanoparticles for Enhanced Oral Absorption

Pharmaceutics ◽  
2018 ◽  
Vol 10 (3) ◽  
pp. 146 ◽  
Author(s):  
Yifan Yang ◽  
Yunzhi Yin ◽  
Jun Zhang ◽  
Tiantian Zuo ◽  
Xiao Liang ◽  
...  
Keyword(s):  
Oral Delivery ◽  
Oral Absorption ◽  
Oral Drug Delivery ◽  
Drug Loading ◽  
In Vitro Release ◽  
Plga Nanoparticles ◽  
Oral Drug ◽  
Average Size ◽  
Promising Perspective

Oral delivery is considered the preferred route of administration due to its convenience and favorable compliance. Here, docetaxel (DTX) loaded polylactic-co-glycolic acid (PLGA) nanoparticles, coated with polyethyleneimine–folic acid (PEI-FA) and polyethyleneimine–borneol (PEI-BO), were designed to enhance oral absorption (FA/BO-PLGA-NPs). The FA/BO-PLGA-NPs were spherical and smooth with an average size of (137.0 ± 2.1) nm. Encapsulation efficiency (EE%) and drug loading (DL%) were (80.3 ± 1.8)% and (2.3 ± 0.3)%, respectively. In vitro release studies showed that approximately 62.1% of DTX was released from FA/BO-PLGA-NPs in media at pH 7.4. The reverted gut sac method showed that the absorption of FA/BO-PLGA-NPs in the intestines was approximately 6.0 times that of DTX. Moreover, cellular uptake suggested that the obtained FA/BO-PLGA-NPs could be efficiently internalized into Caco-2 cells via FA-mediated active targeting and BO-mediated P-glycoprotein (P-gp) inhibition. Pharmacokinetics study demonstrated that after oral administration of DTX at a dose of 10 mg/kg in FA/BO-PLGA-NPs, the bioavailability of FA/BO-PLGA-NPs was enhanced by approximately 6.8-fold compared with that of DTX suspension. FA/BO-PLGA-NPs caused no obvious irritation to the intestines. Overall, the FA/BO-PLGA-NP formulation remarkably improved the oral bioavailability of DTX and exhibited a promising perspective in oral drug delivery.

Thiolated Eudragit-Coated Chitosan Microspheres as an Oral Drug Delivery System

2007 ◽  
Vol 342-343 ◽  
pp. 445-448 ◽  
Author(s):  
Ji Shan Quan ◽  
Hu Lin Jiang ◽  
Yun Jaie Choi ◽  
Mi Kyong Yoo ◽  
Chong Su Cho
Keyword(s):  
Oral Delivery ◽  
Oral Drug Delivery ◽  
In Vitro Release ◽  
Oral Drug ◽  
Average Particle ◽  
Protein Drug ◽  
Chitosan Microspheres ◽  
Oral Drug Delivery System ◽  
Cysteine Hydrochloride

The aim of this study is to prepare mucoadhesive chitosan microspheres for protein drug to deliver to intestine through oral administration. The thiolated Eudragit was synthesized by reaction between L-cysteine hydrochloride and Eudragit® L-100. About 8 mol-% of cysteine was introduced to the Eudragit-cysteine conjugate. The conjugate was used to coat bovine serum albumin (BSA)-loaded chitosan microspheres. The average particle sizes of BSA-loaded thiolated Eudragit-coated chitsoan microspheres (TECMs) were 4.06±0.74 .m and the uniform sizedistribution was shown. The in vitro release of BSA from BSA-loaded TECMs was pH-dependent. Our results indicated that thiolated Eudragit might be a good candidate as a coating material for oral delivery of protein drug owing to mucoadhesive and pH-sensitive properties.

scholarly journals EFFECT OF NATURAL AND SYNTHETIC POLYMERS ON THE PROPERTIES OF CANDESARTAN CILEXETIL MATRIX TABLET PREPARED BY DRY GRANULATION

2016 ◽  
Vol 9 (9) ◽  
pp. 161
Author(s):  
Omar Saeb Salih ◽  
Roaa Abdalhameed Nief
Keyword(s):  
Drug Delivery ◽  
Candesartan Cilexetil ◽  
Oral Drug Delivery ◽  
In Vitro Release ◽  
Oral Drug ◽  
Matrix Tablet ◽  
Sustained Release Formulation ◽  
Weight Variation ◽  
Vitro Release

ABSTRACTObjective: The objective of this study is to develop a controlled release matrix tablet of candesartan cilexetil to reduce the frequency of administration,enhance bioavailability and improve patient compliance; a once daily sustained release formulation of candesartan cilexetil is desirable.Methods: The prepared tablets from F1 to F24 were evaluated with different evaluation parameters like weight variation, drug content, friability,hardness, thickness and swelling ability. In vitro release for all formulas were studied depends on the type and amount of each polymer, i.e. (16 mg,32 mg and 48 mg) respectively beside to the combination effect of polymers on the release of the drug from the tablet.Results: In vitro release showed that formula 13 had the faster release (100% after 4 h) which contained acacia (1:1) and the lowest sustain releasewas showed for F7 (73% after 8 h) which contained HPMC K100M (1:1). Formula 1 was an 89 % release after 8 h which contain eudragit RS100; F4was a 100 % release after 5 h which contain Na CMC, F10 was a 100% after 8 h which contain xanthan gum and F16 was a 100 % release after 5 hwhich contain tragacanth polymer. Formula 9 had a lower release than F7 and F8 respectively. Formula 7 can be used for sustain oral drug delivery ofcandesartan cilexetil while Formula 13 can be used in contrary as fast release tablets for faster response.Conclusion: Controlled drug delivery system is promising for less dosing and higher patient compliance.Keywords: Angiotensin II receptor antagonist, Hypertension, Matrix system, Control release.

DEVELOPMENT AND IN VITRO EVALUATION OF PHYTOSOME OF TERBINAFINE HYDROCHLORIDE FOR ORAL DRUG DELIVERY

2020 ◽  
pp. 85-94
Author(s):  
SHIVAM SHARMA ◽  
VIVEK
Keyword(s):  
Fourier Transforms ◽  
Oral Drug Delivery ◽  
In Vitro Release ◽  
Molar Ratio ◽  
Oral Drug ◽  
In Vitro Evaluation ◽  
Terbinafine Hydrochloride ◽  
Membrane Technique ◽  
Terbinafine Hcl

Objective: The purpose of this study was to develop and in vitro evaluation phytosome of terbinafine HCL to enhance the bioavailability for oral route. Methods: The novel phytosome of terbinafine hydrochloride (TFH) was formulated with the molar ratio (1:2) of drug and phospholipid by using solvent evaporation technique. The resulting TFH-PC was determined by means of particle size analyzer (PSA), percentage yield, microscopy, drug content, transmission electron microscopy (TEM). Substantial contact of terbinafine HCL with phospholipids was completed through Fourier transforms infrared spectroscopy (FTIR). Results: The all relevant results of TFH-PC were showed that the percentage entrapment efficiency of formulation was found in 76% to 90%. In vitro release data were exhibited approximately 65% to 79% of the drug released from the TFH-PC formulation by using dialysis membrane technique. Therefore, Formulation (F3) was accomplished that phytosome contain the superior physical characters and compatibility with drug and phospholipids than to make it easy to overcome the competence of drug to pass the lipid-rich bio-membrane. Conclusion: In present work, terbinafine loaded phytosome was formulated for increasing the oral bioavailability of selected drug. Hence, TER-HCL phytosome were effectively improved the absorption of drug in form of phospholipids complex.

Facile Synthesis of Chitosan Based-(AMPS-co-AA) Semi-IPNs as a Potential Drug Carrier: Enzymatic Degradation, Cytotoxicity, and Preliminary Safety Evaluation

2019 ◽  
Vol 16 (3) ◽  
pp. 242-253 ◽  
Author(s):  
Kaleem Ullah ◽  
Muhammad Sohail ◽  
Abdul Mannan ◽  
Haroon Rashid ◽  
Aamna Shah ◽  
...  
Keyword(s):  
Drug Release ◽  
Oral Drug Delivery ◽  
Drug Carrier ◽  
Drug Loading ◽  
In Vitro Cytotoxicity ◽  
Oral Drug ◽  
Specific Enzyme ◽  
Oral Toxicity ◽  
Scanning Calorimetry

Objective: The study describes the development of chitosan-based (AMPS-co-AA) semi-IPN hydrogels using free radical polymerization technique. Methods: The resulting hydrogels were characterized using Fourier Transform Infrared Spectroscopy (FTIR), Thermogravimetric Analysis (TGA), Differential Scanning Calorimetry (DSC), X-Ray diffraction (XRD), and Scanning Electron Microscopy (SEM). The successful crosslinking of chitosan, 2- Acrylamido-2-Methylpropane Sulfonic Acid (AMPS), and Acrylic Acid (AA) was confirmed by FT IR. Unloaded and drug-loaded hydrogels exhibited higher thermal stability after crosslinking compared to the individual components. XRD confirmed the decrease in crystallinity after hydrogel formation and molecular dispersion of Oxaliplatin (OXP) in the polymeric network. SEM showed rough, vague and nebulous surface resulting from crosslinking and loading of OXP. Results: The experimental results revealed that swelling and drug release were influenced by the pH of the medium being low at acidic pH and higher at basic pH. Increasing the concentration of chitosan and AA enhanced the swelling, drug loading and drug release while AMPS was found to act inversely. Conclusion: It was confirmed that the hydrogels were degraded more by specific enzyme lysozyme as compared to the non-specific enzyme collagenase. In-vitro cytotoxicity suggested that the unloaded hydrogels were non-cytotoxic while crude drug and drug-loaded hydrogel exhibited dose-dependent cytotoxicity against HCT-116 and MCF-7. Results of acute oral toxicity on rabbits demonstrated that the hydrogels are non-toxic up to 3900 mg/kg after oral administration, as no toxicity or histopathological changes were observed in comparison to control rabbits. These pH-sensitive hydrogels appear to provide an ideal basis as a safe carrier for oral drug delivery.

scholarly journals Clarithromycin-Loaded Poly (Lactic-co-glycolic Acid) (PLGA) Nanoparticles for Oral Administration: Effect of Polymer Molecular Weight and Surface Modification with Chitosan on Formulation, Nanoparticle Characterization and Antibacterial Effects

Polymers ◽  
2019 ◽  
Vol 11 (10) ◽  
pp. 1632 ◽  
Author(s):  
A. Alper Öztürk ◽  
Evrim Yenilmez ◽  
Mustafa Güçlü Özarda
Keyword(s):  
Oral Delivery ◽  
Glycolic Acid ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Plga Nanoparticles ◽  
Test Method ◽  
Molecular Weights ◽  
Antibiotic Group ◽  
Surface Modified

Clarithromycin (CLR) is a member of the macrolide antibiotic group. CLR has low systemic oral bioavailability and is a drug of class II of the Biopharmaceutical Classification System. In many studies, using nanoparticles (NPs) as a drug delivery system has been shown to increase the effectiveness and bioavailability of active drug substances. This study describes the development and evaluation of poly (lactic-co-glycolic acid) (PLGA) NPs and chitosan (CS)-coated PLGA NPs for oral delivery of CLR. NPs were obtained by nanoprecipitation technique and characterized in detail, and the effect of three molecular weights (Mw1: 7.000–17.000, Mw2: 38.000–54.000, Mw3: 50.000–190.000) of PLGA and CS coating on particle size (PS), zeta potential (ZP), entrapment efficiency (EE%), and release properties etc. were elucidated. Gastrointestinal stability and cryoprotectant effect tests were performed on the NPs. The PS of the prepared NPs were in the range of 178 to 578 nm and they were affected by the Mw and CS coating. In surface-modified formulations with CS, the ZP of the NPs increased significantly to positive values. EE% varied from 62% to 85%, depending upon the Mw and CS coating. In vitro release studies of CLR-loaded NPs showed an extended release up to 144 h. Peppas–Sahlin and Weibull kinetic model was found to fit best for CLR release from NPs. By the broth microdilution test method, the antibacterial activity of the formulations was determined on Staphylococcus aureus (ATCC 25923), Listeria monocytogenes (ATCC 1911), and Klebsiella pneumoniae (ATCC 700603). The structures of the formulations were clarified by thermal (DSC), FT-IR, and 1H-NMR analysis. The results showed that PS, ZP, EE%, and dissolution rates of NPs were directly related to the Mw of PLGA and CS coating.

Bioadhesive Mannosylated Nanoparticles for Oral Drug Delivery

2006 ◽  
Vol 6 (9) ◽  
pp. 3203-3209 ◽  
Author(s):  
Hesham H. Salman ◽  
Carlos Gamazo ◽  
Miguel A. Campanero ◽  
Juan M. Irache
Keyword(s):  
Drug Delivery ◽  
Oral Delivery ◽  
Oral Drug Delivery ◽  
Normal Mucosa ◽  
Oral Drug ◽  
Con A ◽  
Distribution Profile ◽  
The Given

The aim of this work was to design mannosylated Gantrez® AN nanoparticles (M-NP) and to describe their gut bioadhesive properties in order to develop a promising carrier for future applications in oral drug delivery. For that purpose, the process of the nanoparticles coating with mannosamine was optimized by the incubation of Gantrez® AN nanoparticles with different volumes of mannosamine aqueous solutions at different times. Then, the nanoparticles were characterized by measuring the size, zeta potential, mannosamine content, and concanavalin A (Con A) binding. Furthermore, in vivo quantitative bioadhesion study and kinetic analysis of the bioadhesion curves were performed after oral administration to rats of fluorescently labelled nanoparticles. The selected mannosylated nanoparticles (M-NP1 and M-NP10) were of homogenous sizes (about 300 and 200 nm), negatively charged and successfully coated with 36 and 18 μg mannosamine/mg NP, respectively. In vitro agglutination assay using Con A confirmed the successful coating of nanoparticles with mannosamine. The gut distribution profile of M-NP1 indicated a stronger bioadhesive capacity than M-NP10 and non-mannosylated ones, 1 h post-administration. Interestingly, M-NP1 showed an important ileum tropism where around 20% of the given dose remained adhered. Besides, the kinetic parameters of the bioadhesion profile of M-NP1 indicated their higher bioadhesive capacity with Qmax and AUCadh about 2-times higher than control ones. Moreover, fluorescence microscopy corroborated the stronger interactions of M-NP1 with the normal mucosa and demonstrated a strong uptake of these carriers by Peyer's patches. In conclusion, we propose that mannosylated nanoparticles could be a promising non-live vector for oral delivery strategies.

scholarly journals Polymeric micelles for oral drug delivery: Why and how

2004 ◽  
Vol 76 (7-8) ◽  
pp. 1321-1335 ◽  
Author(s):  
M. F. Francis ◽  
Mariana Cristea ◽  
F. M. Winnik
Keyword(s):  
Drug Delivery ◽  
Oral Delivery ◽  
Oral Absorption ◽  
Polymeric Micelles ◽  
Oral Drug Delivery ◽  
Polymeric Micelle ◽  
Water Soluble ◽  
Oral Drug ◽  
Therapeutic Effects ◽  
The Impact

The oral delivery of drugs is regarded as the optimal means for achieving therapeutic effects owing to increased patient compliance. Unfortunately, the oral delivery route is beset with problems such as gastrointestinal (GI) destruction of labile molecules, low levels of macromolecular absorption, etc. To reduce the impact of digestive enzymes and to ensure the absorption of bioactive agents in an unaltered form, molecules may be incorporated into microparticulate carriers. Many approaches to achieve the oral absorption of a wide variety of drugs are currently under investigation. Among the different polymer-based drug delivery systems, polymeric micelles represent a promising delivery vehicle especially intended for poorly water-soluble pharmaceutical active ingredients in order to improve their oral bioavailability. Recent findings of a dextran-based polymeric micelle study for solubilization of a highly lipophilic drug, cyclosporin A (CsA), will be discussed.

Assessment of Exenatide loaded Biotinylated Trimethylated Chitosan/HP-55 Nanoparticles

2021 ◽  
Vol 18 ◽  
Author(s):  
Hejian Guo ◽  
Xuehui Yan ◽  
Hao Tang ◽  
Xiaoyan Zhang
Keyword(s):  
Oral Administration ◽  
Drug Loading ◽  
Hydroxypropyl Methylcellulose ◽  
In Vitro Release ◽  
Antidiabetic Activity ◽  
Daily Injection ◽  
Oral Drug ◽  
Pharmaceutical Industries ◽  
Vitro Release

Background: Exenatide (EXE) is an anti-hyperglycemic agent approved for treating type 2 diabetes by the Food and Drug Administration (FDA). However, twice-daily injection of exenatide inconveniences most patients. Objective: In this study, biotinylated trimethylated chitosan (Bio-TMC) based nanoparticles were proposed to promote oral absorption of exenatide. Realizing the oral administration of exenatide is very important to alleviate patient suffering and improve patient compliance. Methods: Bio-TMC was synthesized, and the chemical structure was characterized by Fourier transform infrared (FT-IR) spectroscopy and 1H NMR spectroscopy. Nanoparticles were prepared through polyelectrolyte interaction in the presence of sodium tripolyphosphate (TPP) and Hydroxypropyl methylcellulose phthalate (HP-55). The formulations were physically and chemically characterized. In vitro release was investigated in different pH media. In vivo antidiabetic activities of biotin modified and non-biotin modified chitosan were evaluated in db/db mice. Results: EXE-loaded Bio-TMC/HP-55 nanoparticles were spherical in shape with a mean diameter of 156.2 nm and zeta potential of +11.3 mV. The drug loading efficiency and loading contents were 52.38% and 2.08%, respectively. In vitro release revealed that EXE-loaded Bio-TMC/HP-55 nanoparticles were released faster in pH 1.2 than pH 6.8 (63.71% vs. 50.12%), indicating that nanoparticles had enteric characteristics. Antidiabetic activity study revealed that after oral administration to diabetic mice, the relative pharmacological bioavailability (FPharm%) of the biotin modified nanoparticles was found to be 1.27-fold higher compared with the unmodified ones and the hypoglycemic effect was also better. Conclusion: Bio-TMC/HP-55 nanoparticles are feasible as oral drug carriers of exenatide and have the potential to be extended to other drugs that are not readily oral, such as monoclonal antibodies, vaccines, genes, etc., thus, this would be beneficial for pharmaceutical industries. Further research will focus on the biodistribution of Bio-TMC/HP-55 nanoparticles after oral administration.

Polymer-Lipid Hybrid Systems: Scope of Intravenous-To-Oral Switch in Cancer Chemotherapy

2020 ◽  
Vol 10 (2) ◽  
pp. 164-177 ◽  
Author(s):  
Md. Rizwanullah ◽  
Javed Ahmad ◽  
Saima Amin ◽  
Awanish Mishra ◽  
Mohammad Ruhal Ain ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Hybrid Systems ◽  
Patient Compliance ◽  
Cancer Chemotherapy ◽  
Oral Delivery ◽  
Oral Absorption ◽  
Oral Drug Delivery ◽  
Drug Carriers ◽  
Oral Drug ◽  
Oral Switch

Cancer chemotherapeutic administration by oral route has the potential to create “hospitalization free chemotherapy”. Such a therapeutic approach will improve patient compliance and significantly reduce the cost of treatment. In current clinical practice, chemotherapy is primarily carried out by intravenous injection or infusion and leads to various unwanted effects. Despite the presence of oral delivery challenges like poor aqueous solubility, low permeability, drug stability and substrate for multidrug efflux transporter, cancer chemotherapy delivery through oral administration has gained much attention recently due to having more patient compliance compared to the intravenous mode of administration. In order to address the multifaceted oral drug delivery challenges, a hybrid delivery system is conceptualized to merge the benefits of both polymeric and lipid-based drug carriers. Polymer-lipid hybrid systems have presented various significant benefits as an efficient carrier to facilitate oral drug delivery by surmounting the different associated obstacles. This carrier system has been found suitable to overcome the numerous oral absorption hindrances and facilitate the intravenous-to-oral switch in cancer chemotherapy. In this review, we aimed to discuss the different biopharmaceutic challenges in oral delivery of cancer chemotherapy and how this hybrid system may provide solutions to such challenges.

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