scholarly journals Controlled Release of Tazarotene from Magnetically Responsive Nanofiber Patch: Towards More Efficient Topical Therapy of Psoriasis

2021 ◽  
Vol 11 (22) ◽  
pp. 11022
Author(s):  
Natália Andrýsková ◽  
Paul Sourivong ◽  
Melánia Babincová ◽  
Mária Šimaljaková

Electrospun polycaprolactone nanofibers with embedded magnetic nanoparticles were developed for use in the topical delivery of antipsoriatic drugs. To test a hydrophobic drug, a tazarotene has been used, which is an efficient retinoid derivative. Such a smart hyperthermia nanofiber system with self-generated heat from the incorporated magnetic nanoparticles induced drug release in response to on–off switching of alternating magnetic fields for the delivery of tazarotene through the skin, as quantified using Franz cells. This highly efficient external field-controllable system with minimal skin irritation could create a new avenue for the topical therapy of psoriasis.

2016 ◽  
Vol 720 ◽  
pp. 12-16 ◽  
Author(s):  
Takahiko Matsunaga ◽  
Takeshi Yabutsuka ◽  
Shigeomi Takai ◽  
Takeshi Yao

Hydroxyapatite (HAp), a principal component of living bone and teeth, is collecting a lot of attention as a biomaterial owing to its biocompatibility. Also, HAp formed in simulated body fluid (SBF) has flake-like structure and porous body. From these properties, in this study, we fabricated HAp microcapsules encapsulating ibuprofen by attaching the Apatite Nuclei (ANs) on oil droplets containing the ibuprofen and soaking the mixture in SBF. In addition, we evaluated the behavior of drug release from the microcapsules In Vitro.


Author(s):  
Kranthi Kumar Kotta ◽  
L. Srinivas

The present investigation focuses on the development of mucoadhesive tablets of captopril which are designed to prolong the gastric residence time after oral administration. Matrix tablets of captopril were formulated using four mucoadhesive polymers namely guar gum, xanthan gum, HPMC K4M and HPMC K15M and studied for parameters such as weight variation, thickness, hardness, content uniformity, swelling index, mucoadhesive force and in vitro drug release. Tablets formulated Xanthan gum or HPMC K4M with HPMC K15M provide slow release of captopril over period of 12 hr and were found suitable for maintenance portion of oral controlled release tablets. The cumulative % of drug release of formulation F9 and F10 were 90 and 92, respectively. In vitro release from these tablets was diffusion controlled and followed zero order kinetics. The ‘n’ values obtained from the pappas-karsemeyer equation suggested that all the formulation showed drug release by non-fickian diffusion mechanism. Tablets formulated Xanthan gum or HPMC K4M with HPMC K15M (1:1) were established to be the optimum formulation with optimum bioadhesive force, swelling index & desired invitro drug release. This product was further subjected to stability study, the results of which indicated no significant change with respect to Adhesive strength and in vitro drug release study.


Author(s):  
Nirmala Rangu ◽  
Gande Suresh

The present study was aimed to develop once-daily controlled release trilayer matrix tablets of nelfinavir to achieve zero-order drug release for sustained plasma concentration. Nelfinavir trilayer matrix tablets were prepared by direct compression method and consisted of middle active layer with different grades of hydroxypropyl methylcellulose (HPMC), PVP (Polyvinyl Pyrrolidine) K-30 and MCC (Micro Crystalline Cellulose). Barrier layers were prepared with Polyox WSR-303, Xanthan gum, microcrystalline cellulose and magnesium stearate. Based on the evaluation parameters, drug dissolution profile and release drug kinetics DF8 were found to be optimized formulation. The developed drug delivery system provided prolonged drug release rates over a period of 24 h. The release profile of the optimized formulation (DF8) was described by the zero-order and best fitted to Higuchi model. FT-IR studies confirmed that there were no chemical interactions between drug and excipients used in the formulation. These results indicate that the approach used could lead to a successful development of a controlled release formulation of nelfinavir in the management of AIDS.


Author(s):  
Rajesh Dubey ◽  
Udaya K. Chowdary ◽  
Venkateswarlu V.

A controlled release formulation of metoclopramide was developed using a combination of hypromellose (HPMC) and hydrogenated castor oil (HCO). Developed formulations released the drug over 20 hr with release kinetics following Higuchi model. Compared to HCO, HPMC showed significantly higher influence in controlling the drug release at initial as well as later phase. The difference in the influence can be explained by the different swelling and erosion behaviour of the polymers. Effect of the polymers on release was optimized using a face-centered central composite design to generate a predictable design space. Statistical analysis of the drug release at various levels indicated a linear effect of the polymers’ levels on the drug release. The release profile of formulations containing the polymer levels at extremes of their ranges in design space was found to be similar to the predicted release profile


2020 ◽  
Vol 15 ◽  
Author(s):  
Balaji Maddiboyina ◽  
Vikas Jhawat ◽  
Gandhi Sivaraman ◽  
Om Prakash Sunnapu ◽  
Ramya Krishna Nakkala ◽  
...  

Background: Venlafaxine HCl is a selective serotonin reuptake inhibitor which is given in the treatment of depression. The delivery of the drug at a controlled rate can be of great importance for prolonged effect. Objective: The objective was to prepare and optimize the controlled release core in cup matrix tablet of venlafaxine HCl using the combination of hydrophilic and hydrophobic polymers to prolong the effect with rate controlled drug release. Methods: The controlled release core in cup matrix tablets of venlafaxine HCl were prepared using HPMC K5, K4, K15, HCO, IPA, aerosol, magnesium sterate, hydrogenated castor oil and micro crystalline cellulose PVOK-900 using wet granulation technique. Total ten formulations with varying concentrations of polymers were prepared and evaluated for different physicochemical parameters such FTIR analysis for drug identification, In-vitro drug dissolution study was performed to evaluate the amount of drug release in 24 hrs, drug release kinetics study was performed to fit the data in zero order, first order, Hixson–crowell and Higuchi equation to determine the mechanism of drug release and stability studies for 3 months as observed. Results: The results of hardness, thickness, weight variation, friability and drug content study were in acceptable range for all formulations. Based on the In vitro dissolution profile, formulation F-9 was considered to be the optimized extending the release of 98.32% of drug up to 24 hrs. The data fitting study showed that the optimized formulation followed the zero order release rate kinetics and also compared with innovator product (flavix XR) showed better drug release profile. Conclusion: The core-in-cup technology has a potential to control the release rate of freely water soluble drugs for single administration per day by optimization with combined use of hydrophilic and hydrophobic polymers.


2019 ◽  
Vol 9 (3) ◽  
pp. 222-233
Author(s):  
Divya D. Jain ◽  
Namita D. Desai

Background: Adapalene is a promising third generation retinoid used in the topical treatment of acne vulgaris. However, the major drawback associated with conventional topical therapy of Adapalene is the ‘retinoid reaction’ which is dose-dependent and characterized by erythema, scaling and burning sensation at the application sites. Microparticulate drug delivery can play a major role in reducing side effects and providing better patient compliance due to targeted delivery. Methods: Adapalene microparticles were prepared using quasi emulsion solvent diffusion method. The effects of formulation variables including polymer ratios, amounts of emulsifier, drug loading and process variables such as stirring time and speed on the physical characteristics of microparticles were investigated. The developed microparticles were characterized by DSC and SEM. Adapalene microparticles were incorporated into Carbopol 971 NF gel for ease of topical delivery. Results: Adapalene microparticulate topical gel showed sustained drug release over 8 hours in in vitro studies. The amount of drug retained in the rat skin during ex vivo studies was higher in the microparticulate topical gel (227.43 ± 0.83 µg/cm2) as compared to the marketed formulation (81.4 ± 1.11 µg/cm2) after 8 hours indicating localized and sustained drug action that can be useful in treating acne vulgaris. The safety of optimized Adapalene gel determined by skin irritation studies performed on Sprague Dawley rats showed no irritation potential. Conclusion: Microparticles can provide promising carrier systems to deliver Adapalene, improving patient compliance due to enhanced skin deposition, localized and sustained action with reduced associated irritant effects.


Soft Matter ◽  
2019 ◽  
Vol 15 (8) ◽  
pp. 1853-1859 ◽  
Author(s):  
Oliver Werzer ◽  
Stephan Tumphart ◽  
Roman Keimel ◽  
Paul Christian ◽  
Anna Maria Coclite

Temperature-controlled release and study on the effects of the drug–polymer interaction and pH.


2014 ◽  
Vol 1060 ◽  
pp. 45-49
Author(s):  
Kamonrak Cheewatanakornkool ◽  
Pornsak Sriamornsak

The main objective of this study was to fabricate biopolymer-based microbeads, providing enteric properties and controlled release of diclofenac sodium, using layer-by-layer technique. The calcium pectinate microbeads have been designed and coated with chitosan and pectin multilayers. Drug release was performed in simulate gastric fluid (pH 1.2) for 2 hours, followed by pH 6.8 buffer for 8 hours. The effects of chitosan concentration, number of layer and drying technique on drug release were investigated. The results showed that the calcium pectinate microbeads could be simply prepared by ionotropic gelation and then coated with chitosan and pectin solutions using layer-by-layer procedure. The diameter of the microbeads ranged from 800 to 1000 μm for air-dried samples and from 1 to 2 mm for freeze-dried samples. The freeze-dried microbeads had a rough surface and many pores inside, as observed by SEM. The microbeads coated with 4% chitosan/4% pectin revealed a slower drug release than those coated with 1% chitosan/4% pectin and demonstrated a controlled release pattern. Moreover, different drying techniques and numbers of layer also influenced drug release behavior of the prepared microbeads.


2013 ◽  
Vol 813 ◽  
pp. 399-402
Author(s):  
Chimsook Thitipha ◽  
Thitiphan Chimsook

The aim of present work was to prepare floating microsphere of ketoprofen using matrix polymer of chitosan and poly (ethylene glycol) by solvent diffusion method. The floating microsphere of ketoprofen was prepared from matrix polymer of chitosan and poly (ethylene glycol) with various composition ratios and evaluated such as particle size, drug compatibility and drug release of microspheres. The scanning electron microscopy of microspheres confirmed their hollow structures with smooth surface. Formulation CPK 4 to CPK 6 exhibited the best controlled release pattern in ketoprofen. The concentration and size of poly (ethylene-glycol) affected the particle size, percentage yield and drug release of microspheres.


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