scholarly journals Nanoemulsion for Solubilization, Stabilization, and In Vitro Release of Pterostilbene for Oral Delivery

2014 ◽  
Vol 15 (4) ◽  
pp. 1000-1008 ◽  
Author(s):  
Yue Zhang ◽  
Zhenhua Shang ◽  
Chunhui Gao ◽  
Man Du ◽  
Shixia Xu ◽  
...  
Keyword(s):  
Oral Delivery ◽  
In Vitro Release ◽  
Vitro Release

Development, in vitro and in vivo Evaluations of Solid-Lipid Microparticles based on Solidified Micellar Carrier System for Oral Delivery of Cefepime

2017 ◽  
Vol 10 (1) ◽  
pp. 3582-3593
Author(s):  
Chukwuebuka Umeyor ◽  
Uchechukwu Nnadozie ◽  
Anthony Attama
Keyword(s):  
Oral Delivery ◽  
In Vitro Release ◽  
Carrier System ◽  
Solid Lipid ◽  
Solid Lipid Microparticles ◽  
Release Study ◽  
Lipid Microparticles ◽  
Vitro Release

This study seeks to formulate and evaluate a solid lipid nanoparticle-based, solidified micellar carrier system for oral delivery of cefepime. Cefepime has enjoyed a lot of therapeutic usage in the treatment of susceptible bacterial infections; however, its use is limited due to its administration as an injection only with poor patient compliance. Since oral drug administration encourage high patient compliance with resultant effect in improved therapy, cefepime was formulated as solid lipid microparticles for oral delivery using the concept of solidified micellar carrier system. The carrier system was evaluated based on particle yield, particle size and morphology, encapsulation efficiency (EE %), and thermal analysis using differential scanning calorimeter (DSC). Preliminary microbiological studies were done using gram positive and negative bacteria. In vitro release study was performed using biorelevant media, while in vivo release study was performed in white albino rats. The yield of solid lipid microparticles (SLM) ranged from 84.2 – 98.0 %. The SLM were spherical with size ranges of 3.8 ± 1.2 to 42.0 ± 1.4 µm. The EE % calculated ranged from 83.6 – 94.8 %. Thermal analysis showed that SLM was less crystalline with high potential for drug entrapment. Microbial studies showed that cefepime retained its broad spectrum anti-bacterial activity. In vitro release showed sustained release of cefepime from SLM, and in vivo release study showed high concentration of cefepime released in the plasma of study rats. The study showed that smart engineering of solidified micellar carrier system could be used to improve oral delivery of cefepime.

scholarly journals Self microemulsifying powder using Aerosil as a carrier

2021 ◽  
Vol 56 (2) ◽  
pp. 141-146
Author(s):  
N Arju ◽  
PK Bara ◽  
MT Amin ◽  
DR Bhowmik ◽  
MS Hossain
Keyword(s):  
Oral Delivery ◽  
Evaluation Studies ◽  
In Vitro Release ◽  
Study Drug ◽  
Evaluation Study ◽  
Flowing Powder ◽  
Uv Visible ◽  
Short Time ◽  
Vitro Release

This investigation highlighted the development of a solid self micro emulsifying drug delivery system (solid SMEDDS) for improved oral delivery of Valsartan. Liquid SMEDDS were formulated and then the liquid formulation was transformed into free-flowing powder by adsorption on a solid carrier. Here the formulations were prepared in various ratios of the drug to the excipients. Various evaluation studies were performed. In-vitro release profiles of all formulations were evaluated. The concentration of the diffused drug was measured using a UV-visible spectrophotometer at λmax= 250 nm. The faster dissolution was exhibited by the formulations containing Avicel. The experimental results for prepared solid-SMEDDS showed the improved dissolution of the study drug in a short time. F-3 (Assay:77%; Dissolution: 51.7% after 45 min, 63% after 60 min) and F-4 (Assay:63%; Dissolution: 49.1% after 45 min, 67% after 60 min) showed better evaluation study and this two might be formulated in future. Thus, this study revealed the formulation solid-SMEDDS using Aerosil 200 as an adsorbent with the potential of enhancing the solubility, and dissolution rate of the drug. Bangladesh J. Sci. Ind. Res.56(2), 141-146, 2021

scholarly journals Optimizing Prednisolone Loading into Distiller’s Dried Grain Kafirin Microparticles, and In vitro Release for Oral Delivery

Pharmaceutics ◽  
2017 ◽  
Vol 9 (4) ◽  
pp. 17 ◽  
Author(s):  
Esther T. L. Lau ◽  
Stuart K. Johnson ◽  
Barbara A. Williams ◽  
Deirdre Mikkelsen ◽  
Elizabeth McCourt ◽  
...  
Keyword(s):  
Oral Delivery ◽  
In Vitro Release ◽  
Vitro Release

scholarly journals Development and Evaluation of Matrix Type Transdermal Patches of Torasemide

2020 ◽  
Vol 10 (5) ◽  
pp. 98-104
Author(s):  
Ashish Kumar ◽  
Kapil Kumar
Keyword(s):  
Oral Delivery ◽  
Loop Diuretic ◽  
In Vitro Release ◽  
Oral Route ◽  
Stability Studies ◽  
Transdermal Patches ◽  
Sulfonyl Urea ◽  
Release Data ◽  
Vitro Release

TDDS manufacture has numerous benefits over other routes like oral delivery. It avoids limitations linked with g.i.t. absorption, enzyme effect, interaction with drug and food. This route is suitable when patient is suffering from vomiting and diarrhea. Torasemide is a loop diuretic; it comes under category of sulfonyl urea. It is prescribed in the treatment of edema, CHF, and hypertension.  Whenever it is used by oral route, it is associated with many side effects like vomiting, nausea, anorexia, and increased appetite. All transdermal patches were transparent and free from any particle. Release profile of twelve batches of Torasemide was done by the means of Franz cell for 7 hrs. Maximum release was shown by MTP6 (71.28±0.19) and least in formulations of batch code MTP7(24.47±0.04). In-vitro release data were plotted in 2 different models i.e. first and Korsemeyer peppas. It was observed that release was governed by the diffusion process. On basis of different properties MTP1 batch was found to be optimum. Study concludes that by the means of patches Torasemide can be administered efficiently. Keywords: Torasemide, transdermal patches, HPMC, in-vitro release, stability studies, TDDS.

Preparation, characterization, and in vitro release of new transdermal methimazole as alternative to oral delivery

Drug Delivery ◽  
2009 ◽  
Vol 16 (1) ◽  
pp. 1-10 ◽  
Author(s):  
M. E. Morales ◽  
B. Clarés ◽  
M. López-Viota ◽  
M. A. Ruiz
Keyword(s):  
Oral Delivery ◽  
In Vitro Release ◽  
Vitro Release

Enhanced Pharmacokinetic Activity of Zotepine via Nanostructured Lipid Carrier System in Wistar Rats for Oral Application

2020 ◽  
Vol 8 (2) ◽  
pp. 148-160 ◽  
Author(s):  
Cernam Tirumalesh ◽  
Dinesh Suram ◽  
Narendar Dudhipala ◽  
Nagaraj Banala
Keyword(s):  
Oral Bioavailability ◽  
Oral Delivery ◽  
Wistar Rats ◽  
Water Solubility ◽  
In Vitro Release ◽  
Log P ◽  
Nanostructured Lipid Carrier ◽  
Vitro Release ◽  
Sem Studies

Background: Zotepine (ZT) is a substituted dibenzothiepine tricyclic molecule and second generation antipsychotic drug. It is available as the parenteral and oral solid dosage form, but, orally administered ZT has a poor oral bioavailability (10%) that might be due to either poor water solubility, high lipophilicity (Log P 4) and also first-pass hepatic metabolism. Objective: The oral bioavailability of ZT was improved by loading into a nanostructured lipid carriers (NLCs) system. Methods: Hot homogenization with probe sonication method was used for the preparation of ZT-NLCs formulations and characterized for an optimal system based on physicochemical characteristics and in vitro release. Differential scanning calorimetry (DSC), X-ray diffraction (XRD) analysis, and scanning electron microscopy (SEM) studies were used to confirm the crystalline nature and shape of the optimized ZT-NLC formulation. The physical stability of the optimized ZT-NLC formulation was evaluated at the refrigerator and room temperature over two months. Furthermore, in vivo pharmacokinetic (PK) studies of optimized ZT-NLC and ZT coarse suspension (ZT-CS) as control formulation, were conducted in male Wistar rats. Results: The optimized formulation of ZT-NLC showed Z-avg, PDI, ZP of 145.8 ± 2.5 nm, 0.18 ± 0.05, -31.6 ± 1.8 mV, respectively. In vitro release studies indicated the sustained release of ZT. DSC and XRD studies revealed the conversion of ZT into an amorphous form. SEM studies showed the spherical shape of the ZT-NLC formulation. PK studies showed 1.8-folds improvement (p<0.05) in oral bioavailability when compared with ZTCS formulation. Conclusion: Overall, the results established that NLCs could be used as a new alternative delivery vehicle for the oral delivery of ZT.

scholarly journals Antitumor efficacy of Folic Acid conjugated Polymeric Nanoparticles of SN-38 after oral delivery

2019 ◽  
Vol 9 (4-s) ◽  
pp. 322-331
Author(s):  
Prasad Shilpi ◽  
J.S Dangi
Keyword(s):  
Particle Size ◽  
Folic Acid ◽  
Oral Delivery ◽  
Tumor Regression ◽  
Polymeric Nanoparticles ◽  
In Vitro Release ◽  
Colon Tumor ◽  
Irinotecan Hydrochloride ◽  
Vitro Release

The objective of the present research was to develop folic acid conjugated polymeric nanoparticles (FCsPNP) and to investigate its therapeutic effectiveness in xenograft Colon tumor models after oral delivery. Chitosan coated PLGA nanoparticles (CsPNP) were prepared by polyelectrolyte complexation method and it was further conjugated with Folic acid. Optimized formulation was investigated for particle size, zeta potential, polydispersity index (PdI), % entrapment drug loading and in vitro release. The morphology was observed by SEM and TEM images. Tumor regression studies were conducted on Balb/c mice implanted with Colo-26 cells. FCsPNP were successfully prepared and optimized. In vitro parameters viz. Particle size, Zeta potential, PdI were found to be optimum. The in vitro % release is directly correlated with the nature of polymers and folate conjugation. In vivo tumor regression studies found the formulations to be less toxic than Irinotecan hydrochloride (IHCl). CsPNP and FCsPNP were successfully prepared and evaluated for antitumor efficacy after oral delivery. FCsPNP were more effective in the colon tumor treatment and found to be less toxic than IHCl thus making it a potential drug delivery candidate for future anticancer therapy. Keywords: Nanoparticles, Xenograft colon tumor, Chitosan, Irinotecan hydrochloride

Development and in vitro and in vivo evaluations of a microemulsion formulation for the oral delivery of oxaprozin

2021 ◽  
Vol 18 ◽  
Author(s):  
Fangming Yin ◽  
Shu Meng ◽  
Xin Zhao ◽  
Huining Wang ◽  
Yingkai Ning ◽  
...  
Keyword(s):  
Particle Size ◽  
Oral Delivery ◽  
Oral Absorption ◽  
In Vitro Release ◽  
Tween 20 ◽  
Peak Time ◽  
Microemulsion Formulation ◽  
Vitro Release

Background: Oxaprozin is labeled as a Class II drug in the biopharmaceutical classification system, and its poor solubility in the entire gastrointestinal tract may be the main reason for its poor oral absorption capacity. Objective: The purpose of this study was to develop an oxaprozin formulation to enhance its oral absorption. Method: Oxaprozin-loaded microemulsions were prepared using the titration method and pseudoternary phase diagram. Characterization experiments were performed on microemulsion preparations, including pH, particle size, shape, zeta potential and stability (thermodynamic, dilution, and differential scanning calorimetry). Then, the in vitro release of the microemulsion and in vivo pharmacokinetics in rats were evaluated. Results : Several microemulsion formulations were prepared. The optimal formulation was 15% oleoyl macrogolglycerides, 35% Tween 20/isopropanol (Km=2) and 50% distilled water. Its particle size met the requirements, and it had a spherical shape with a negatively charged surface. This microemulsion-loaded drug was applied to in vitro release and in vivo pharmacokinetic experiments at 7.47 mg/mL. In vitro release of the oxaprozin-loaded microemulsion best fit the first-order model, while the microemulsion preparation had a certain sustained release effect. In vivo pharmacokinetic experiments indicated that the microemulsion formulation significantly delayed the peak time of the blood concentration and simultaneously prolonged the half-life of drug elimination. Conclusions : The obtained data revealed satisfactory results for this novel microemulsion of oxaprozin, which is very meaningful for clinical trials.

scholarly journals Enhancement of Oral Bioavailability of Puerarin by Polybutylcyanoacrylate Nanoparticles

2011 ◽  
Vol 2011 ◽  
pp. 1-8 ◽  
Author(s):  
Lixia Zhao ◽  
Anchang Liu ◽  
Min Sun ◽  
Jinsong Gu ◽  
Haigang Wang ◽  
...  
Keyword(s):  
Zeta Potential ◽  
Oral Bioavailability ◽  
Oral Delivery ◽  
Drug Carrier ◽  
In Vitro Release ◽  
Spherical Shape ◽  
Oral Drug ◽  
Burst Release ◽  
Vitro Release

The interest using novel drug delivery systems to improve oral bioavailability of drug with poor solubility is increasing. In this study, a new oral delivery system, polybutylcyanoacrylate nanoparticles (PBCNs), was introduced to improve the oral bioavailability of puerarin (PUE). PUE-loaded PBCN was successfully prepared by anionic polymerization method. Characterization of PUE-loaded PBCN was evaluated with morphology, size, zeta potential, and in vitro release study. The PBCN loading PUE exhibited a spherical shape under transmission electron microscopy with an average size of 159.4 nm, and the zeta potential was −15.0 mV. The in vitro release of PUE-loaded PBCN showed an initial burst release followed by a sustained release. Physicochemical state of PUE in PBCN was investigated by differential scanning colorimetry, X-ray diffraction, and Fourier transform infrared spectroscopy. The results indicated that PUE in PBCN was in a noncrystalline state. The oral pharmacokinetic study in rats showed that the relative bioavailability of PUE-encapsulated PBCN to the crude PUE was more than 550%. It can be concluded that PBCN as an oral drug carrier can significantly improve the oral bioavailability of PUE.

Sign in / Sign up

Export Citation Format

Share Document