Preparation and Characterization of Biopolymeric Nanoparticles as Drug Delivery Vehicles

Author(s):  
Sai S. Sagiri ◽  
Suraj K. Nayak ◽  
S. Lakshmi ◽  
Kunal Pal

In recent years, the use of biopolymeric nanoparticles as vehicles for drug delivery has increased exponentially. In the present study, chitosan and gelatin nanoparticles were prepared by ionic gelation and desolvation methods, respectively. Salicylic acid was used as the model drug. The nanoparticles were characterized using SEM, XRD analysis and FTIR spectrophotometric studies. In vitro drug release experiments were carried out to understand the mechanism of drug release. SEM micrographs showed the formation of spherical nanoparticles. XRD studies indicated a higher crystalline nature of the chitosan nanoparticles as compared to the gelatin nanoparticles. FTIR studies indicated the presence of salicylic acid within the drug- loaded nanoparticles. Drug release studies indicated that the developed nanoparticles may be used as carriers for various bioactive agents.

Author(s):  
Sai S. Sagiri ◽  
Suraj K. Nayak ◽  
S. Lakshmi ◽  
Kunal Pal

In recent years, the use of biopolymeric nanoparticles as vehicles for drug delivery has increased exponentially. In the present study, chitosan and gelatin nanoparticles were prepared by ionic gelation and desolvation methods, respectively. Salicylic acid was used as the model drug. The nanoparticles were characterized using SEM, XRD analysis and FTIR spectrophotometric studies. In vitro drug release experiments were carried out to understand the mechanism of drug release. SEM micrographs showed the formation of spherical nanoparticles. XRD studies indicated a higher crystalline nature of the chitosan nanoparticles as compared to the gelatin nanoparticles. FTIR studies indicated the presence of salicylic acid within the drug- loaded nanoparticles. Drug release studies indicated that the developed nanoparticles may be used as carriers for various bioactive agents.


2012 ◽  
Vol 455-456 ◽  
pp. 901-906
Author(s):  
Kui Lin Deng ◽  
Chun Yuan Huang ◽  
Xiao Bo Ren ◽  
Yu Bo Gou ◽  
Hai Bin Zhong ◽  
...  

A novel pH-sensitive poly (2-(acryloyloxy) propanoic acid) hydrogel (PAPA) synthesized from lactic acid by radical polymerization has been investigated in this work. The structure of prepared monomer2-(acryloyloxy) propanoic acid) (APA) has been characterized by FTIR and1H-NMR measurements. PAPA hydrogel demonstrated an obvious pH sensitivity in its swelling in the range of 4-7 pH of phosphate buffer solution (PBS). The rapid response of the hydrogel makes it suitable for drug delivery application. Here, salicylic acid (SA) selected as a model drug, thein-vitrodrug release as a function of pH and temperature was studied systematically. The cumulative release of salicylic acid reached up to 86.6% in pH=7.4 PBS at 37.0°C within 550min. In pH=2.1 PBS, however, only 26.6% drug was released from the pH-sensitive PAPA on the same conditions.


Polymers ◽  
2019 ◽  
Vol 11 (11) ◽  
pp. 1834 ◽  
Author(s):  
Ullah ◽  
Khan ◽  
Choi ◽  
Kim

: This work demonstrates a simple approach for coating a porous polymer layer on stainless-steel (SS) microneedles characterized by a pH-responsive formulation for self-regulated drug delivery. For many drug-delivery applications, the release of therapeutic agents in an acidic microenvironment is desirable. Acid-sensitive polymers and hydrogels were extensively explored, but easily prepared polymeric microcarriers that combine acid sensitivity and biodegradability are rare. Here, we describe a simple and robust method of coating a porous polymer layer on SS microneedles (MNs) that release a model drug (lidocaine) in a pH-responsive fashion. It was constructed by packing the model drug and a pH-sensitive component (sodium bicarbonate) into the pores of the polymer layer. When this acid-sensitive formulation was exposed to the acidic microenvironment, the consequent reaction of protons (H+) with sodium bicarbonate (NaHCO3) yielded CO2. This effect generated pressure inside the pores of the coating and ruptured the thin polymer membrane, thereby releasing the encapsulated drug. Scanning electron micrographs showed that the pH-sensitive porous polymer-coated MNs exposed to phosphate-buffered saline (PBS) at pH 7.4 were characterized by closed pores. However, MNs exposed to PBS at pH 5.5 consisted of open pores and the thin membrane burst. The in vitro studies demonstrated the pH sensitivity of the drug release from porous polymer-coated MNs. Negligible release was observed for MNs in receiving media at pH 7.4. In contrast, significant release occurred when the MNs were exposed to acidic conditions (pH 5.5). Additionally, comparable results were obtained for drug release in vitro in porcine skin and in PBS. This revealed that our developed pH-responsive porous polymer-coated MNs could potentially be used for the controlled release of drug formulations in an acidic environment. Moreover, the stimuli-responsive drug carriers will enable on-demand controlled release profiles that may enhance therapeutic effectiveness and reduce systemic toxicity.


2017 ◽  
Vol 25 (3) ◽  
pp. 241-246 ◽  
Author(s):  
Neha Mulchandani ◽  
Nimish Shah ◽  
Tejal Mehta

Chitosan is a natural polymer obtained from exoskeletons of crustaceans and polyvinyl alcohol (PVA) is a synthetic polymer which has excellent film forming ability along with non-toxic nature. The current work focuses on synthesizing a smart polymer by copolymerization of natural and synthetic polymers and exploring its applications in drug delivery. The copolymers were blended in different ratios and were synthesized using ammonium ceric nitrate as initiator and glutaraldehyde as a crosslinking agent which were converted to films by casting method. Amoxicillin, as a model drug was incorporated to the copolymerized films to study the in-vitro drug release. The films obtained were evaluated by varying the pH to study the pH responsive nature of films. Drug release studies were performed to obtain the release profile of drug; water uptake capacity of the copolymerized film were measured to determine the swelling behaviour of the films. The films were further characterized using Fourier Transform Infrared Spectroscopy (FTIR), Scanning Electron Microscopy (SEM) and Differential Scanning Calorimetry (DSC) to identify the structural and morphological changes along with thermal transitions. The results indicate that the synthesized copolymers are pH responsive in nature having great potential for application in controlled and targeted drug delivery.


2021 ◽  
pp. 088532822110122
Author(s):  
Esmaeil Salimi ◽  
Mohammad Jafar Molaei

This study aimed to provide a new drug delivery system for hydrophobic compounds. Dexamethasone (DEX) was employed as a hydrophobic model drug, which incorporated into the network of hydroxyapatite (HA)/Cyclodextrin (β-CD) nanocomposite. Phase analysis, chemical bonding, morphology, and drug release was evaluated using XRD, FTIR, FESEM, and UV-vis spectroscopy, respectively. XRD patterns showed the formation of the crystalline structure and FTIR analysis showed the chemical bonding between organic and inorganic phases. FESEM images accompanied by EDX analysis confirmed the presence of HA nano-flakes. Release of DEX loaded β-CD/HA was measured to be around 4.6% and 18.7% in pH5.3 and pH 7.4, respectively. In conclusion, the prepared system could be a potential pH sensitive carrier for sustainable release of water-insoluble drugs.


2020 ◽  
Vol 19 (05) ◽  
pp. 1950036
Author(s):  
V. Lavanya ◽  
P. Rajeswari ◽  
M. Vidyavathi ◽  
R. V. Sureshkumar

This study is aimed at the preparation and evaluation of atorvastatin (AN)-loaded chitosan (CS) nanoparticles to achieve improved bioavailability of atorvastatin as its bioavailability is very poor. Chitosan is a popular choice in the application as a drug delivery carrier due to its biocompatibility, chemical versatility, aqueous solubility and low cost. Hence, a total of nine formulations (AN1–AN9) were prepared to study the effects of CS:tripolyphosphate (TPP) ratio and the amount of drug. The best formulation was selected by calculating the overall desirability (OD) factor. Among all, AN9 was found to possess the maximum percentage yield, loading efficiency and percentage (%) drug release compared to other formulations due to the incorporation of more amount of polymer compared to other formulations. SEM microphotographs and zeta-sizer reports indicated that atorvastatin-loaded chitosan nanoparticles were in the nanometric range and were spherical, discrete and uniform in size. The selected polymer chitosan was found to possess good compatibility with atorvastatin, without any mutual interaction, based on the results of DSC and FTIR analyses. The nanoparticles were found to have good flow properties. The in vivo results proved that the best formulation has shown significant difference in the reduction of triglycerides (TG), total cholesterol (TC) and no significant change in high density lipids (HDL) cholesterol levels in blood when compared with the marketed formulation. Better regenerative changes were observed during histopathological evaluation of liver in a group treated with atorvastatin nanoparticles than those of other groups, that confirmed the improved hypolipidemic action. Thus, from all the above observations, it was concluded that AN9 formulation has shown the highest in vitro drug release and loading efficiency than other formulations, which might be due to increased entrapment of drug and the surface area through decreased particle size which further confirmed the improved in vitro bioavailability and in vivo performance than those of marketed atorvastatin tablet. This study strongly suggests the use of chitosan nanoparticles as drug delivery system to improve the bioavailability of atorvastatin.


2011 ◽  
Vol 117-119 ◽  
pp. 1227-1230
Author(s):  
Kui Lin Deng ◽  
Ting Gao ◽  
Yu Bo Gou ◽  
Wei Wang ◽  
Peng Fei Zhang ◽  
...  

In this paper, a new pH/temperature sensitive beads with core-shelled structure, composed of sodium alginate and poly(N-acryloylglycinate), were prepared using as drug delivery carrier. Selecting indomethacin as a model drug, in vitro drug release behaviors were investigated at different temperatures, phosphate buffer solutions (PBS) and polymer content. At pH=2.1, the release amount of indomethacin loaded in the beads was only 2.46% while this value approached to 95.23% in pH=7.4 PBS. In addition, the release rate of indomethacin at 37°C is much higher than at 18°C.


2019 ◽  
Vol 9 (1) ◽  
pp. 6-8
Author(s):  
Rajkumari Thagele

Cancer has become a solemn threat to the life of human beings universally. Various strategies are available to steadfastness cancer; however they are not so effective owed to their serious side effects, noxious effect to healthy cells and non- specificity to cancer cells targeting. To tenacity above facts we try to deed inherent characters of cancer cells. HA was used as a targeting agent for drug delivery to breast cancer cells. In this work nanoparticles were equipped using chitosan and sodium tripolyphosphate encapsulating methotrexate. Methotrexate (Mtx) a folic acid antagonist that inhibits dihydrofolatereductase (DHFR) and blocks conversion of dihydrofolic acid (DHFA) to tetrahydrofolic acid (THFA) of the cell cycle. Chitosan anchored nanoparticles were prepared by ionotropic gelation method by means of sodium tripolyphosphate and evalauted for in-vitro drug release study with dialysis membrane. Result depicts that drug releases from chitosan nanoparticles in sustained manner over a prolonged episode of time from the NPs as the medium acidity enhanced at the target site, not in plasma. In conclusion, chitosan anchored nanoparticles of MTX could be well thought-out as probable candidate for drug delivery in the treatment of breast cancer. Keywords: Breast cancer, Methotrexate, Chitosan, TPP and Nanoparticles.


2012 ◽  
Vol 2012 ◽  
pp. 1-8 ◽  
Author(s):  
M. J. Barea ◽  
M. J. Jenkins ◽  
Y. S. Lee ◽  
P. Johnson ◽  
R. H. Bridson

A novel liposome-in-microsphere (LIM) formulation has been created comprising drug-loaded liposomes within pH responsive Eudragit S100 microspheres. The liposomes contained the model drug 5-ASA and were coated with chitosan in order to protect them during encapsulation within the microspheres and to improve site-specific release characteristics.In vitrodrug release studies showed that LIMs prevented drug release within simulated stomach and small intestine conditions with subsequent drug release occurring in large intestine conditions. The formulation therefore has potential for oral colonic drug delivery.


Author(s):  
Pravin Patil ◽  
Anil Sharma ◽  
Subhash Dadarwal ◽  
Vijay Sharma

The objective of present investigation was to enhance brain penetration of Lamivudine, one of the most widely used drugs for the treatment of AIDS. This was achieved through incorporating the drug into solid lipid nanoparticles (SLN) prepared by using emulsion solvent diffusion technique. The formulations were characterized for surface morphology, size and size distribution, percent drug entrapment and drug release. The optimum rotation speed, resulting into better drug entrapment and percent yield, was in the range of 1000-1250 r/min. In vitro cumulative % drug release from optimized SLN formulation was found 40-50 % in PBS (pH-7.4) and SGF (pH-1.2) respectively for 10 h. After 24 h more than 65 % of the drug was released from all formulations in both mediums meeting the requirement for drug delivery for prolong period of time.


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