scholarly journals Polymer/Iron-Based Layered Double Hydroxides as Multifunctional Wound Dressings

Pharmaceutics ◽  
2020 ◽  
Vol 12 (11) ◽  
pp. 1130
Author(s):  
Mariana Pires Figueiredo ◽  
Ana Borrego-Sánchez ◽  
Fátima García-Villén ◽  
Dalila Miele ◽  
Silvia Rossi ◽  
...  
Keyword(s):  
Drug Release ◽  
High Performance ◽  
Mechanical Performance ◽  
Release Kinetics ◽  
Wound Dressings ◽  
In Vitro Drug Release ◽  
Improved Performance ◽  
Double Hydroxide ◽  
Double Hydroxides

This work presents the development of multifunctional therapeutic membranes based on a high-performance block copolymer scaffold formed by polyether (PE) and polyamide (PA) units (known as PEBA) and layered double hydroxide (LDH) biomaterials, with the aim to study their uses as wound dressings. Two LDH layer compositions were employed containing Mg2+ or Zn2+, Fe3+ and Al3+ cations, intercalated with chloride anions, abbreviated as Mg-Cl or Zn-Cl, or intercalated with naproxenate (NAP) anions, abbreviated as Mg-NAP or Zn-NAP. Membranes were structurally and physically characterized, and the in vitro drug release kinetics and cytotoxicity assessed. PEBA-loading NaNAP salt particles were also prepared for comparison. Intercalated NAP anions improved LDH–polymer interaction, resulting in membranes with greater mechanical performance compared to the polymer only or to the membranes containing the Cl-LDHs. Drug release (in saline solution) was sustained for at least 8 h for all samples and release kinetics could be modulated: a slower, an intermediate and a faster NAP release were observed from membranes containing Zn-NAP, NaNAP and Mg-NAP particles, respectively. In general, cell viability was higher in the presence of Mg-LDH and the membranes presented improved performance in comparison with the powdered samples. PEBA containing Mg-NAP sample stood out among all membranes in all the evaluated aspects, thus being considered a great candidate for application as multifunctional therapeutic dressings.

Formulation and Evaluation of Transdermal patch of Methimazole

2021 ◽  
pp. 4667-4672
Author(s):  
Nani Tadhi ◽  
Himansu Chopra ◽  
Gyanendra Kumar Sharma
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Transdermal Patch ◽  
Formulation Development ◽  
In Vitro Drug Release ◽  
Drug Release Study ◽  
Percent Moisture ◽  
Release Study

Transdermal patch is a drug delivery device in which the drugs are incorporated and is design in such a way that it releases the drug in sustained and at predetermined rate to deliver the drug through the skin to the systemic circulation painlessly. The aim of this research study was to formulate a controlled and sustained release transdermal matrix type patch of Methimazole. The matrix patch was prepared by solvent casting method using a various polymer in different concentration, HPMC (hydrophilic), Eudragit RL100 and Ethyl cellulose (hydrophobic) polymer. Total 9 prototype formulation were prepared and it was subjected for various evaluation test; weight uniformity, Folding endurance, thickness, Drug content, percent moisture content, percent Moisture uptake and In-vitro drug release study using Franz diffusion cell. The in-vitro CDR% data was fit into kinetics model to see the release kinetics from the patches. The Formulation F5 was choosen as a best formulation according to in-vitro drug release study. The in-vitro release was found 81.12 % in 12 hours, it followed zero order kinetics. The nature of polymer and concentration ratio of polymers plays a crucial role for obtaining a good transdermal patch design; therefore optimisation is very important step to formulate a desired TDDS. Therefore the result of the study encourages a further study and is hopeful that the present study would contribute to the recent pharmaceutical research for formulation development.

Fabrication and Release Kinetics of Liposomes Containing Leuprolide Acetate

2021 ◽  
Vol 7 (1) ◽  
pp. 35-38
Author(s):  
Sudipta Das ◽  
Arnab Samanta ◽  
Koushik Bankura ◽  
Debatri Roy ◽  
Amit Nayak
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Zero Order ◽  
Leuprolide Acetate ◽  
Lipid Film ◽  
In Vitro Drug Release ◽  
Liposomal Formulations ◽  
Kinetics Of

The present work is focused on the preparation and in vitro release kinetics of liposomal formulation of Leuprolide Acetate. In this work, “Thin Lipid Film Hydration Method” was used for preparation of Leuprolide Acetate loaded liposomes. Prepared liposomal formulations of Leuprolide acetate was evaluated by drug entrapment study, in-vitro drug release kinetics and stability studies. The percentage drug entrapment of Leuprolide acetate for F1 and F2 formulations were found to be 78.14 ± 0.67 and 66.70 ± 0.81% respectively. In-vitro drug release study of liposomal formulations had shown zero order release pattern. Regression co-efficient (R2) value of Zero order kinetics for F1 and F2 formulations were 0.9912 and 0.9676 respectively. After storing formulations for 1 month, stability testing was done at 40C.It was found that all batches were stable. These liposomal formulations of Leuprolide acetate can be formulated for parenteral application to treat prostate cancer and in women, to treat symptoms of endometriosis (overgrowth of uterine lining outside of the uterus) or uterine fibroids.

scholarly journals Optimizing the Role of Polymer Blend in the Preparation of Acyclovir Controlled-Release Tablets: An Approach for Better Patient Compliance

2018 ◽  
Author(s):  
Barkat Khan ◽  
Faheem Haider ◽  
Kifayat Shah ◽  
Bushra Uzair ◽  
Kaijian Hou ◽  
...  
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Release Kinetics ◽  
Immediate Release ◽  
Matrix Tablets ◽  
Release Mechanism ◽  
In Vitro Drug Release ◽  
Solubility Study ◽  
Release Data

This study was carried out to formulate and evaluate controlled release (CR) matrix tablets of Acyclovir using combination of hydrophilic and hydrophobic polymers. Acyclovir is a guanine derivative and is its half-life is short hence administered five times a day using immediate release tablets. Six formulations (F1-F6) were developed using Ethocel and Carbopol in equal combinations at drug-polymer (D:P) ratio of 10:5, 10:6, 10:7, 10:8, 10:9 and 10:10. Solubility study was performed using six different solvents. The compatibility studies were carried out using FTIR and DSC. According to USP, Quality Control and dimensional tests (hardness, friability, disintegration and thickness) were executed. In-vitro drug release studies of Acyclovir was carried out in dissolution apparatus using using 0.1 N HCl medium at constant temperature of 37 ± 0.5 ºC. In order to analyze the drug release kinetics, five different mathematical models were applied to the release data. The results showed that there was no incompatibility between drug and polymers. Physical QC tests were found within limits of USP. The release was retarded upto 24 hrs and non-fickian in-vitro drug release mechanism was found. A formulation developed using blend of polymers, showed excellent retention and desired release profiles thus providing absolute control for 24 hrs.

FORMULATION AND EVALUATION OF NATEGLINIDE NANOSPONGES

INDIAN DRUGS ◽  
2018 ◽  
Vol 55 (02) ◽  
pp. 27-35
Author(s):  
A. A Bakliwal ◽  
◽  
D. S. Jat ◽  
S. G. Talele ◽  
A. G. Jadhav
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Release Kinetics ◽  
Synthesis Method ◽  
Ultra Sound ◽  
Size Analysis ◽  
Release Kinetic ◽  
In Vitro Drug Release ◽  
Drug Content

The objective of the present study was to produce extended release nateglinide nanosponges for oral delivery. Preparation of nanosponges leads to solubility enhancement. Nateglinide is a BCS Class II drug, having low solubility. So, to increase the solubility of nateglinide it is formulated into nanosponges. Nanosponges using ethyl cellulose as a polymer and dichloromethane as a cross-linker were prepared successfully by ultra-sound assisted synthesis method. The effects of different drug: placebo ratios on the physical characteristics of the nanosponges as well as the drug content and in vitro drug release of the nanosponges were investigated. Particle size analysis and surface morphology of nanosponges were performed. The scanning and transmission electron microscopy of nanosponges showed that they were spongy in nature. The particle size was found to be in the range 46.37 - 97.23 nm out of which particle size of the optimized formulation was 51.79 nm and the drug content was found to 79.43 %. The optimized nanosponge formulations were selected for preparing nanosponge tablets for extended drug delivery by oral route. These tablets were prepared using xanthan gum and PVP K-30 and were evaluated by pre-compression and post-compression parameters. The nateglinide nanosponges tablet formulation were studied for different parameters using Design Expert Software. All formulations were evaluated for in vitro drug release analyzed according to various release kinetic models and it was found that it follows zero order release kinetics.

scholarly journals The ALGINATE MICROSPHERES CONTAINING CURCUMIN: PREPARATION, CHARACTERIZATION, AND IN VITRO HUMAN HAEMOGLOBIN GLYCOSYLATION ASSAY

2019 ◽  
pp. 221-225
Author(s):  
KULKARNI AS ◽  
BHUJBAL SS
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Therapeutic Potential ◽  
Release Kinetics ◽  
Glycosylated Hemoglobin ◽  
Scanning Electron Micrographs ◽  
In Vitro Drug Release ◽  
Human Haemoglobin ◽  
Scanning Electron

Objective: The objective of the present study was to formulate, evaluate alginate microspheres of curcumin, and to investigate the inhibitory effect on glycosylated hemoglobin. Methods: All formulations were prepared by an ionotropic gelation technique using sodium alginate as a polymer and calcium chloride as a crosslinker in varying concentrations. The formulation batches (F1–F6) were evaluated for physical properties such as compatibility studies, percentage entrapment efficiency (%EE), microsphere yield, particle size, and polydispersity index. In vitro, drug release was studied and surface morphology was characterized by scanning electron microscopy. Results: The microspheres showed %EE, microsphere yield, particle size in the ranges of 44.86%–84.24%, 43.05%–81.4%, and 352–559 μm, respectively. In vitro, drug release and release kinetics showed that the developed curcumin microspheres system is a promising delivery system for controlled drug release. Scanning electron micrographs indicate porous and rough surface. The inhibitory properties of curcumin and microspheres (F4) on glycosylation formation were investigated in hemoglobin using quercetin as standard. The decreased in hemoglobin concentration after incubation of hemoglobin with a graded concentration of glucose over a specified time was used as an index for in vitro human hemoglobin glycosylation assay. Glycosylation inhibition was about 75% for standard quercetin, 60% for curcumin microspheres, and 38.74% for curcumin suspension occurred after 72 h. Conclusion: From these results, it can be concluded that curcumin in microsphere formulation has better therapeutic potential and could prove to be useful in the development of antidiabetic formulation.

scholarly journals In vitro study of sirolimus release from nonwoven PLLA matrices

2018 ◽  
Vol 4 (1) ◽  
pp. 591-594
Author(s):  
Sabine Illner ◽  
Stefanie Kohse ◽  
Claudia Michaelis ◽  
Thomas Reske ◽  
Niels Grabow ◽  
...  
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Volume Ratio ◽  
In Vitro Study ◽  
Complete Wetting ◽  
In Vitro Drug Release ◽  
Spray Coatings ◽  
Plasma Pretreatment ◽  
Predetermined Time

AbstractSirolimus incorporated nonwoven polymer matrices were fabricated via electrospinning. Release kinetics considering different fiber diameters and layer thicknesses were investigated. In vitro drug release profiles were evaluated by measuring the drug concentration in an established drug release medium (0.9% saline solution with additives, not buffered) at predetermined time points. Furthermore, an NH3-plasma pretreatment was examined to ensure complete wetting from the beginning of the study. In comparison to thin drug-loaded PLLA spray coatings it was shown that the release of sirolimus is diffusion- and degradation-controlled regardless of the surface-to-volume ratio, though fiber diameters or a hydrophilization can affect its release kinetics.

scholarly journals PREPARATION, CHARACTERISATION AND EVALUATION OF ROPINIROLE HYDROCHLORIDE LOADED CONTROLLED RELEASE MICROSPHERES USING SOLVENT EVAPORATION TECHNIQUE

2018 ◽  
Vol 10 (6) ◽  
pp. 57
Author(s):  
Koyel Kar ◽  
R. N. Pal ◽  
N. N. Bala
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Release Kinetics ◽  
Drug Loading ◽  
Solvent Evaporation ◽  
In Vitro Drug Release ◽  
Aqueous Solvent ◽  
Evaporation Technique ◽  
Ropinirole Hydrochloride

Objective: The major objective of the research work was to design, characterise and evaluate controlled release microspheres of ropinirole hydrochloride by using non-aqueous solvent evaporation technique to facilitate the delivery of the drug at a predetermined rate for a specific period of time.Methods: Ropinirole hydrochloride microspheres were prepared by using different low-density polymers such as eudragit RL 100, eudragit RS 100 and ethylcellulose either alone or in combination with the help of non-aqueous solvent evaporation technique. All the formulated microparticles were subjected to various evaluation parameters such as particle size analysis, micrometric properties, drug entrapment efficiency, percentage drug loading, percentage yield and in vitro drug release study. The compatibility of the drug and polymers was confirmed by physical compatibility study, fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and x-ray diffraction study (XRD). The formation of the most optimized batch of the microsphere (F12) was confirmed by scanning electron microscopy (SEM), DSC, FTIR, and XRD. In vitro drug release study and in vitro drug release kinetics study of the formulated microspheres were also carried out.Results: Drug-polymer compatibility studies performed with the help of FTIR and DSC indicated that there were no interactions. Results revealed that non-aqueous solvent evaporation technique was a suitable technique for the preparation of microspheres as most of the formulations were discrete, free-flowing and spherical in shape with a good yield of 55.67% to 80.09%, percentage drug loading of 35.52% to 94.50% and percentage drug entrapment efficiency of 36.24% to 95.07%. Different drug-polymer ratios, as well as the combination of polymers, played a significant role in the variation of over-all characteristics of formulations. Based on the data of various evaluation parameters such as particle size analysis, percentage drug loading, percentage drug entrapment, percentage yield, rheological studies and in vitro drug release characteristics, formulation F12 was found to fulfil the criteria of ideal controlled release drug delivery system. F12 showed controlled release till the 14th hour (97.99%) and its in vitro release kinetics was best explained by zero-order kinetics and followed Korsemeyer-Pappas model (Non-Fickian mechanism). SEM of F12 revealed the formation of spherical structures. The FTIR study of F12 confirmed the stable nature of ropinirole in the drug-loaded microspheres. DSC and XRD patterns showed that ropinirole hydrochloride was dispersed at the molecular level in the polymer matrix.Conclusion: The controlled release microparticles were successfully prepared and from this study, it was concluded that the developed microspheres of ropinirole hydrochloride can be used for controlled drug release to improve the bioavailability and patient compliance and to maintain a constant drug level in the blood target tissue by releasing the drug in zero order pattern.

scholarly journals FORMULATION AND EVALUATION OF RAMIPRIL MOUTH DISSOLVING FILMS

2019 ◽  
pp. 124-129
Author(s):  
Jasvanth E ◽  
Teja D ◽  
Mounika B ◽  
Buchi N Nalluri
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Hydroxypropyl Methylcellulose ◽  
Release Mechanism ◽  
Onset Of Action ◽  
In Vitro Drug Release ◽  
Drug Release Mechanism ◽  
Preparation And Evaluation ◽  
Pvp K30

Objective: The present investigation was aimed at preparation and evaluation of mouth dissolving films (MDFs) of Ramipril to enhance patient convenience, compliance and to improve bioavailability. Methods: MDFs with 0.5% w/w Ramipril were prepared by a solvent casting method using a wet film applicator. The effects of film formers, wetting/solubilizing, saliva stimulating agents and film modifiers on the physicomechanical and in vitro Ramipril release from MDFs were evaluated. Results: The MDFs prepared were transparent, smooth and showed no re-crystallization upon storage. MDFs casted with hydroxypropyl methylcellulose (HPMC) E3 as film former and polyethylene glycol (PEG-400) as plasticizer showed superior Ramipril release rates and good physicomechanical properties when compared to MDFs with E5 and E15 as film formers. HPMC E3 MDFs with polyvinyl pyrrolidone K30 (PVP K30) and sodium lauryl sulphate (SLS) gave superior drug release properties than MDFs without PVP K30 and SLS. The HPMC E3 MDFs with citric acid (CA) as saliva stimulating and xylitol as soothing agent gave significantly superior in vitro drug release than the MDFs without CA and xylitol. Release kinetics data reveals diffusion as a drug release mechanism. Conclusion: From the obtained results, it can be concluded that the administration of Ramipril as MDF may provide a quick onset of action with enhanced oral bioavailability and therapeutic efficacy.

scholarly journals Formulation and Evaluation of Tacrolimus Transdermal Gel

2019 ◽  
Vol 9 (6-s) ◽  
pp. 110-118
Author(s):  
CH. Suryakumari ◽  
M. Narender ◽  
K. Umasankar ◽  
Siva Prasad Panda ◽  
S.N. Koteswara Rao ◽  
...  
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Release Kinetics ◽  
In Vitro Drug Release ◽  
Surface Ph ◽  
Abdominal Skin ◽  
Ex Vivo Permeation ◽  
Ex Vivo Permeation Study ◽  
Carbopol 934P

The present investigation is concerned with formulation and evaluation of Transdermal gels of Tacrolimus, anti-psoriasis drug, to circumvent the first pass effect and to improve its bioavailability with reduction in dosing frequency and dose related side effects. Twelve formulations were developed with varying concentrations of polymers like Carbopol 934P, HPMCK4M and Sodium CMC. The gels were tested for clarity, Homogeneity, Spreadability, Extrudability, Viscosity, surface pH, drug Content uniformity, in-vitro drug diffusion study and ex-vivo permeation study using rat abdominal skin. FTIR studies showed no evidence on interactions between drug, polymers and excipients. The best in-vitro drug release profile was achieved with the formulation F4 containing 0.5 mg of exhibited 6 hr drug release i.e. 98.68 % with desired therapeutic concentration which contains the drug and Carbopol 934p in the ratio of 1:2. The surface pH, drug content and viscosity of the formulation F4 was found to be 6.27, 101.3% and 3, 10,000cps respectively. The drug permeation from formulation F4 was slow and steady and 0.89gm of tacrolimus could permeate through the rat abdominal skin membrane with a flux of 0.071 gm hr-1 cm-2. The in-vitro release kinetics studies reveal that all formulations fit well with zero order kinetics followed by non-Fickian diffusion mechanism. Keywords: Transdermal gel, Viscosity, In-vitro drug release, In-vitro drug release kinetics study, Ex-vivo permeation study

scholarly journals Development and Characterization of Ofloxacin & Prednisolone Loaded Nanostructured Lipid Carriers (Nlc) for Topical Route

2019 ◽  
Vol 4 (1) ◽  
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Release Kinetics ◽  
Morphological Characteristics ◽  
Nanostructured Lipid Carriers ◽  
Diffusion Method ◽  
Prolonged Release ◽  
In Vitro Drug Release ◽  
Drug Content

Aim: The present study was designed to develop and characterize nanostructured lipid carriers (NLC) of Ofloxacin and Prednisolone for topical use in case of infections associated with inflammation. Materials and Methods: Ofloxacin was obtained as gift sample from Mankind Pharma Ltd, VillKyarta, P.O. Misserwal, Poonta Sahib, Sir Mour. H.P. Whereas Prednisolone was purchased from Yarrow chem., Mumbai. It was evaluated for its pre-formulation studies (organoleptic properties, melting point, solubility, compatibility, max. wavelength of absorption). NLCs were prepared through melt-emulsification followed by ultra-sonication technique. Further optimized batch of NLCs was incorporated into Gel. Formulated NLCs were evaluated in terms of morphological characteristics, particle size (Polydispersity Index), drug content, In-vitro drug release (using egg membrane), drug release kinetics (Ritger-Peppas diffusion method). Finally, gel containing NLCs was studied by physical characteristics, pH, viscosity, spreadability, drug content, In-vitro drug release and its kinetics. Results and Discussion: In pre-formulation study, drugs were found having the similar properties as described in Indian Pharmacopoeia (IP) and United States Pharmacopoeia (USP). SEM photomicrograph revealed that NLCs were spherical with more or less smooth surface; particle size 512.3-1703 nm and PDI- 0.399-0.742 (ofloxacin) and particle size 539.3-1736.7 nm and PDI- 0.335 - 0.711 (prednisolone);drug content was found in range of 56.7 - 75.6% for ofloxacin and 65.9 – 81.8% for prednisolone. NLC1 demonstrated maximum release rate with 83.37±1.70% and NLC8 73.96±0.53%.NLC6 was best fitted in Korsmeyer - peppas model as the regression coefficients were 0.960, 0.964, 0.977, 0.950, 0.980 & 0.987 respectively and prednisolone NLC 9 (0.953) and they were close to 1. Conclusion: In conclusion, the prepared NLCs had prolonged release effects with good potential for topical delivery of NLC based gel formulation of ofloxacin& prednisolone.

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