scholarly journals HPMC- and PLGA-Based Nanoparticles for the Mucoadhesive Delivery of Sitagliptin: Optimization and In Vivo Evaluation in Rats

Materials ◽  
2019 ◽  
Vol 12 (24) ◽  
pp. 4239 ◽  
Author(s):  
Anroop B. Nair ◽  
Nagaraja Sreeharsha ◽  
Bandar E. Al-Dhubiab ◽  
Jagadeesh G. Hiremath ◽  
Pottathil Shinu ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Delivery System ◽  
Oral Therapy ◽  
Ex Vivo ◽  
Narrow Particle Size Distribution ◽  
Drug Content ◽  
Prepared Nanoparticles

Mucoadhesive nanoparticles represent a potential drug delivery strategy to enhance the therapeutic efficacy in oral therapy. This study assessed the prospective of developing HPMC- and PLGA-based nanoparticles using a nanospray drier as a mucoadhesive extended release drug delivery system for sitagliptin and evaluated their potential in an animal model. Nanoparticles were prepared using a Buchi® B-90 nanospray drier. Optimization of particle size was performed using response surface methodology by examining the influence of spray-drying process variables (inlet temperature, feed flow, and polymer concentration) on the particle size. The prepared nanoparticles were characterized for various physicochemical characteristics (yield, drug content, morphology, particle size, thermal, and crystallographic properties) and assessed for drug release, stability, and mucoadhesive efficacy by ex vivo and in vivo studies in rats. A linear model was suggested by the design of the experiments to be the best fit for the generated design and values. The yield was 77 ± 4%, and the drug content was 90.5 ± 3.5%. Prepared nanoparticles showed an average particle size of 448.8 nm, with a narrow particle size distribution, and were wrinkled. Thermal and crystallographic characteristics showed that the drug present in the nanoparticles is in amorphous dispersion. Nanoparticles exhibited a biphasic drug release with an initial rapid release (24.9 ± 2.7% at 30 min) and a prolonged release (98.9 ± 1.8% up to 12 h). The ex vivo mucoadhesive studies confirmed the adherence of nanoparticles in stomach mucosa for a long period. Histopathological assessment showed that the formulation is safe for oral drug delivery. Nanoparticles showed a significantly higher (p < 0.05) amount of sitagliptin retention in the GIT (gastrointestinal tract) as compared to control. The data observed in this study indicate that the prepared mucoadhesive nanoparticles can be an effective alternative delivery system for the oral therapy of sitagliptin.

Development and Evaluation of Floating Pulsatile Drug Delivery System Using Meloxicam

2017 ◽  
Vol 7 (04) ◽  
Author(s):  
ShirishaG. Suddala ◽  
S. K. Sahoo ◽  
M. R. Yamsani
Keyword(s):  
Rheumatoid Arthritis ◽  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Lag Time ◽  
Oral Dosage ◽  
Lag Phase ◽  
Pulsatile Drug Delivery

Objective: The objective of this research work was to develop and evaluate the floating– pulsatile drug delivery system (FPDDS) of meloxicam intended for Chrono pharmacotherapy of rheumatoid arthritis. Methods: The system consisting of drug containing core, coated with hydrophilic erodible polymer, which is responsible for a lag phase for pulsatile release, top cover buoyant layer was prepared with HPMC K4M and sodium bicarbonate, provides buoyancy to increase retention of the oral dosage form in the stomach. Meloxicam is a COX-2 inhibitor used to treat joint diseases such as osteoarthritis and rheumatoid arthritis. For rheumatoid arthritis Chrono pharmacotherapy has been recommended to ensure that the highest blood levels of the drug coincide with peak pain and stiffness. Result and discussion: The prepared tablets were characterized and found to exhibit satisfactory physico-chemical characteristics. Hence, the main objective of present work is to formulate FPDDS of meloxicam in order to achieve drug release after pre-determined lag phase. Developed formulations were evaluated for in vitro drug release studies, water uptake and erosion studies, floating behaviour and in vivo radiology studies. Results showed that a certain lag time before drug release which was due to the erosion of the hydrophilic erodible polymer. The lag time clearly depends on the type and amount of hydrophilic polymer which was applied on the inner cores. Floating time and floating lag time was controlled by quantity and composition of buoyant layer. In vivo radiology studies point out the capability of the system of longer residence time of the tablets in the gastric region and releasing the drug after a programmed lag time. Conclusion: The optimized formulation of the developed system provided a lag phase while showing the gastroretension followed by pulsatile drug release that would be beneficial for chronotherapy of rheumatoid arthritis and osteoarthritis.

In Vitro and In Vivo Drug Release from a Novel In Situ Forming Drug Delivery System

2007 ◽  
Vol 25 (6) ◽  
pp. 1347-1354 ◽  
Author(s):  
Heiko Kranz ◽  
Erol Yilmaz ◽  
Gayle A. Brazeau ◽  
Roland Bodmeier
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
In Situ Forming

scholarly journals Novel concept of the smart NIR-light–controlled drug release of black phosphorus nanostructure for cancer therapy

2018 ◽  
Vol 115 (3) ◽  
pp. 501-506 ◽  
Author(s):  
Meng Qiu ◽  
Dou Wang ◽  
Weiyuan Liang ◽  
Liping Liu ◽  
Yin Zhang ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Cancer Therapy ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Near Infrared ◽  
Black Phosphorus ◽  
Deep Penetration ◽  
Nir Light

A biodegradable drug delivery system (DDS) is one the most promising therapeutic strategies for cancer therapy. Here, we propose a unique concept of light activation of black phosphorus (BP) at hydrogel nanostructures for cancer therapy. A photosensitizer converts light into heat that softens and melts drug-loaded hydrogel-based nanostructures. Drug release rates can be accurately controlled by light intensity, exposure duration, BP concentration, and hydrogel composition. Owing to sufficiently deep penetration of near-infrared (NIR) light through tissues, our BP-based system shows high therapeutic efficacy for treatment of s.c. cancers. Importantly, our drug delivery system is completely harmless and degradable in vivo. Together, our work proposes a unique concept for precision cancer therapy by external light excitation to release cancer drugs. If these findings are successfully translated into the clinic, millions of patients with cancer will benefit from our work.

scholarly journals Development of Piperine-Loaded Solid Self-Nanoemulsifying Drug Delivery System: Optimization, In-Vitro, Ex-Vivo, and In-Vivo Evaluation

Nanomaterials ◽  
2021 ◽  
Vol 11 (11) ◽  
pp. 2920
Author(s):  
Ameeduzzafar Zafar ◽  
Syed Sarim Imam ◽  
Nabil K. Alruwaili ◽  
Omar Awad Alsaidan ◽  
Mohammed H. Elkomy ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Delivery ◽  
Ex Vivo ◽  
In Vitro Release ◽  
System Optimization ◽  
Globule Size

Hypertension is a cardiovascular disease that needs long-term medication. Oral delivery is the most common route for the administration of drugs. The present research is to develop piperine self-nanoemulsifying drug delivery system (PE-SNEDDS) using glyceryl monolinoleate (GML), poloxamer 188, and transcutol HP as oil, surfactant, and co-surfactant, respectively. The formulation was optimized by three-factor, three-level Box-Behnken design. PE-SNEDDs were characterized for globule size, emulsification time, stability, in-vitro release, and ex-vivo intestinal permeation study. The optimized PE-SNEDDS (OF3) showed the globule size of 70.34 ± 3.27 nm, percentage transmittance of 99.02 ± 2.02%, and emulsification time of 53 ± 2 s Finally, the formulation OF3 was transformed into solid PE-SNEDDS (S-PE-SNEDDS) using avicel PH-101 as adsorbent. The reconstituted SOF3 showed a globule size of 73.56 ± 3.54 nm, PDI of 0.35 ± 0.03, and zeta potential of −28.12 ± 2.54 mV. SEM image exhibited the PE-SNEDDS completely adsorbed on avicel. Thermal analysis showed the drug was solubilized in oil, surfactant, and co-surfactant. S-PE-SNEDDS formulation showed a more significant (p < 0.05) release (97.87 ± 4.89% in 1 h) than pure PE (27.87 ± 2.65% in 1 h). It also exhibited better antimicrobial activity against S. aureus and P. aeruginosa and antioxidant activity as compared to PE dispersion. The in vivo activity in rats exhibited better (p < 0.05) antihypertensive activity as well as 4.92-fold higher relative bioavailability than pure PE dispersion. Finally, from the results it can be concluded that S-PE-SNEDDS might be a better approach for the oral delivery to improve the absorption and therapeutic activity.

A Smart Drug Delivery System Based on Thermo-Responsive Polymer Gated Au NRs@SiO2 Nano-Platform

2021 ◽  
Vol 16 (7) ◽  
pp. 1029-1036
Author(s):  
Hongzhu Wang ◽  
Mengxun Chen ◽  
Liping Song ◽  
Youju Huang
Keyword(s):  
Drug Delivery ◽  
Block Copolymer ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Photothermal Therapy ◽  
Drug Loading ◽  
Temperature Sensitive

A key challenge for nanoparticles-based drug delivery system is to achieve manageable drug release in tumour cell. In this study, a versatile system combining photothermal therapy and controllable drug release for tumour cells using temperature-sensitive block copolymer coupled Au NRs@SiO2 is reported. While the Au NRs serve as hyperthermal agent and the mesoporous silica was used to improve the drug loading and decrease biotoxicity. The block copolymer acted as “gatekeeper” to regulate the release of model drug (Doxorubicin hydrochloride, DOX). Through in vivo and in vitro experiments, we achieved the truly controllable drug release and photothermal therapy with the collaborative effect of the three constituents of the nanocomposites. The reported nanocomposites pave the way to high-performance controllable drug release and photothermal therapy system.

scholarly journals Formulation and evaluation of solid self micro emulsifying drug delivery system using aerosil 200 as solid carrier

2012 ◽  
Vol 1 (12) ◽  
pp. 414-419 ◽  
Author(s):  
Durgacharan Arun Bhagwat ◽  
John Intru D’Souza
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Intestinal Permeability ◽  
Delivery System ◽  
Ex Vivo ◽  
Water Soluble ◽  
Solid Carrier ◽  
Drug Content ◽  
Permeability Study ◽  
Poorly Water Soluble

Improvement of bio-availability of poorly water soluble drugs presents one of the furthermost challenge in drug formulations. One of the most admired and commercially viable formulation approach for this challenge is solid self micro emulsifying drug delivery system (S-SMEDDS). There are many techniques to convert liquid SMEDDS to solid, but an adsorption technique is simple and economic. Hence aim of present study was to develop S-SMEDDS of poorly water soluble drug Telmisartan (TEL) using Aerosil 200 as solid carrier. Liquid SMEDDS was prepared using Acrysol EL 135, Tween 80 and PEG 400 as oil, surfactant and co-surfactant and was converted to S-SMEDDS by adsorbing it on Aerosil 200. Prepared S-SMEDDS was evaluated for flow properties, drug content, reconstitution properties, DSC, SEM, in-vitro drug release and ex-vivo intestinal permeability study. Results showed that prepared S-SMEDDS have good flow property with 99.45 ± 0.02% drug content. Dilution study by visual observation showed that there was spontaneous micro emulsification and no sign of phase separation. Droplet size was found to be 0.34 µm with polydispersity index of 0.25. DSC thermogram showed that crystallization of TEL was inhibited. SEM photograph showed smooth surface of S-SMEDDS with less aggregation. Drug releases from S- SMEDDS were found to be significantly higher as compared with that of plain TEL. Ex-vivo intestinal permeability study revealed that diffusion of drug was significantly higher from S-SMEDDS than that of suspension of plain TEL. Study concluded that S-SMEDDS can effectively formulated by adsorption technique with enhanced dissolution rate and concomitantly bioavailability.DOI: http://dx.doi.org/10.3329/icpj.v1i12.12451 International Current Pharmaceutical Journal 2012, 1(12): 414-419

scholarly journals Docetaxel-loaded Poly(3HB-co-4HB) Biodegradable Nanoparticles: Impact of Co-polymer Composition

2020 ◽  
Author(s):  
Faisalina Ahmad Fisol ◽  
Fabio Sonvico ◽  
Paolo Colombo ◽  
Amirul Al-Ashraf Abdullah ◽  
Habibah A. Wahab ◽  
...  
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Particle Size Distribution ◽  
Size Distribution ◽  
Water Soluble ◽  
Polymer Composition ◽  
Narrow Particle Size Distribution ◽  
Wide Range ◽  
Polymer Ratio

Polyhydroxyalkanoate (PHA) co-polymers show relatively higher in vivo degradation rate compared to other PHAs thus they received a great deal of attention for a wide range of medical applications. Nanoparticles (NPs) loaded with poorly water soluble anticancer drug docetaxel (DCX) were produced using poly 3-hydroxybutyrate-co-4-hydroxybutyrate, P(3HB-co-4HB), co-polymers biosynthesised from Cupriavidus sp. USMAA1020 isolated from Malaysian environment. Three co-polymers with different molar proportions of 4-hydroxybutirate (4HB) were used: 16% (PHB16), 30% (PHB30) and 70% (PHB70) 4HB-containing P(3HB-co-4HB). Blank and DCX loaded nanoparticles were then characterized for their size and size distribution, surface charge, encapsulation efficiency and drug release. Pre-formulation studies showed that an optimised formulation could be achieved through the emulsification/solvent evaporation method using PHB70 with the addition of 1.0% PVA, as stabilizer and 0.03% VitE-TPGS, as surfactant. DCX-loaded PHB70 nanoparticles (DCX-PHB70) gave the desired particle size distribution in term of average particles sizes around 150 nm and narrow particle size distribution (PDI below 0.100). The encapsulation efficiencies result showed that at 30% w/w drug-to-polymer ratio: DCX- PHB16 NPs were able to encapsulate up to 42% of DCX; DCX-PHB30 NPs encapsulated up to 46% of DCX and DCX-PHB70 NPs encapsulated up to 50% of DCX within the nanoparticles system. Approximately 60% of DCX was released from the DCX-PHB70 NPs within 7 days for 5%, 10% and 20% of drug to polymer ratio while for the 30% and 40% drug to polymer ratios, an almost complete drug release (98%) after 7 days of incubation was observed.

scholarly journals Laser-activated drug implant for controlled release to the posterior segment of the eye

2020 ◽  
Author(s):  
Xingyu He ◽  
Zheng Yuan ◽  
Samantha Gaeke ◽  
Winston W.-Y. Kao ◽  
S. Kevin Li ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Posterior Segment ◽  
Zero Order ◽  
First Order ◽  
Drug Implants

AbstractThe current standard of care for posterior segment eye diseases, such as age-related macular degeneration and diabetic macular edema, is frequent intravitreal injections or sustained-release drug implants. Drug implants have side effects due to the burst release of the drugs, and their release cannot be easily controlled after implantation. Present study attempts to develop a dosage-controllable drug delivery implant which consists of a nanoporous biodegradable PLGA capsule and light-activated liposomes. Controllable drug release from the implant was achieved by using pulsed near-infrared (NIR) laser both in vitro and in vivo. The in vitro drug release kinetics from two different initial dose implants, 1000 μg and 500 μg, was analyzed by fitting zero order and first order kinetics, as well as the Korsmeyer-Peppas and Higuchi models. The 1000 μg and 500 μg implants fit the first-order and zero-order kinetics model, respectively, the best. The multiple drug releases in the vitreous was determined by in vivo fluorimeter, which was consistent with the in vitro data. The dose released was also clinically relevant. Histology and optical and ultrasound imaging data showed no abnormality in the eyes received implant treatment suggesting that the drug delivery system was safe to the retina. This on-demand dose-controllable drug delivery system could be potentially used for long-term posterior eye disease treatment.

scholarly journals DESIGN, PREPARATION, AND EVALUATION OF SELF-MICROEMULSIFYING DRUG DELIVERY SYSTEM OF BAMBUTEROL HYDROCHLORIDE

2019 ◽  
pp. 332
Author(s):  
SACHIN SAGGAR ◽  
ASHUTOSH UPADHAYAY ◽  
MANISH GOSWAMI
Keyword(s):  
Drug Delivery ◽  
Phase Diagram ◽  
Drug Delivery System ◽  
Delivery System ◽  
Ternary Phase Diagram ◽  
Ex Vivo ◽  
The Self ◽  
Drug Content ◽  
Intestinal Membrane ◽  
Globule Size

Objective: The self-micro-emulsifying drug delivery system (SMEDDS) of bambuterol hydrochloride was designed, prepared, and evaluated to overcome the problem of poor bioavailability. Methods: The designing of the formulation included the selection of oil phase, surfactant, and cosolvent/cosurfactant based on the saturated solubility studies. Psuedoternary phase diagram was constructed using aqueous titration method, to identify the self-emulsifying region. Different ratios of the selected surfactant and cosolvent/cosurfactant (Smix) were also studied and used to construct the ternary phase diagram. The prepared formulations of the SMEDDS were evaluated for drug content, morphology, globule size, robustness to dilution, emulsification time, optical clarity, and stability. Results: The formulation containing 10 mg bambuterol hydrochloride, triacetin (12.50% w/w), Tween 80 (43.75% w/w), and ethanol (43.75% w/w) was concluded to be optimized. The optimized SMEDDS not only showed optimum globule size, zeta potential, and drug content but was also found to be robust to dilution, formed emulsion spontaneously, and was stable. The optimized SMEDDS showed increased permeability of the drug across the intestinal membrane in ex vivo studies. Conclusion: The results suggest that bambuterol hydrochloride can be formulated as self-microemulsifying drug delivery system, and further, SMEDDS can be used to improve the oral bioavailability of bambuterol hydrochloride.

Formulation and evaluation of resveratrol loaded cubosomal nanoformulation for topical delivery

2020 ◽  
Vol 17 ◽  
Author(s):  
Bhaskar Kurangi ◽  
Sunil Jalalpure ◽  
Satveer Jagwani
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Topical Application ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Drug Permeation

Aim: The aim of the study was to formulate, characterize, and evaluate the resveratrol-loaded cubosomes (RC) through topical application. Background: Resveratrol (RV) is a nutraceutical compound that has exciting pharmacological potential in different diseases including cancers. Many studies of resveratrol have been reported for anti-melanoma activity. Due to its low bioavailability, the activities of resveratrol are strongly limited. Hence, an approach with nanotechnology has been done to increase its activity through transdermal drug delivery. Objective: To formulate, characterize, and evaluate the resveratrol-loaded cubosomes (RC). To evaluate resveratrol-loaded cubosomal gel (RC-Gel) for its topical application. Methods: RC was formulated by homogenization technique and optimized using a 2-factor 3-level factorial design. Formulated RCs were characterized for particle size, zeta potential, and entrapment efficiency. Optimized RC was evaluated for in vitro release and stability study. Optimized RC was further formulated into cubosomal gel (RC-Gel) using carbopol and evaluated for drug permeation and deposition. Furthermore, developed RC-Gel was evaluated for its topical application using skin irritancy, toxicity, and in vivo local bioavailability studies. Results: The optimized RC indicated cubic-shaped structure with mean particle size, entrapment efficiency, and zeta potential were 113±2.36 nm, 85.07 ± 0.91%, and -27.40 ± 1.40 mV respectively. In vitro drug release of optimized RC demonstrated biphasic drug release with the diffusion-controlled release of resveratrol (RV) (87.20 ± 2.25%). The RC-Gel demonstrated better drug permeation and deposition in mice skin layers. The composition of RC-Gel has been proved non-irritant to the mice skin. In vivo local bioavailability study depicted the good potential of RC-Gel for skin localization. Conclusion: The RC nanoformulation proposes a promising drug delivery system for melanoma treatment simply through topical application.

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