A novel nanoparticles impregnated ocular insert for enhanced bioavailability to posterior segment of eye: In vitro, in vivo and stability studies

2017 ◽  
Vol 71 ◽  
pp. 529-540 ◽  
Author(s):  
Lalaji V. Rathod ◽  
Rakhee Kapadia ◽  
Krutika K. Sawant
Keyword(s):  
Posterior Segment ◽  
Stability Studies ◽  
Ocular Insert

scholarly journals Formulation and In Vitro-In Vivo Correlation of Timolol Maleate Ocular Insert

2015 ◽  
Vol 4 (4) ◽  
pp. 281-288 ◽  
Author(s):  
Sunil Thakral ◽  
◽  
Roshan Issarani ◽  
Badri P. Nagori ◽  
◽  
...  
Keyword(s):  
Timolol Maleate ◽  
Ocular Insert

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 Preparation of Fluconazole -Cyclodextrin Complex Ocuserts: In Vitro and In Vivo Evaluation

2011 ◽  
Vol 2011 ◽  
pp. 1-8 ◽  
Author(s):  
Hindustan Abdul Ahad ◽  
J. Sreeramulu ◽  
B. Suma Padmaja ◽  
M. Narasimha Reddy ◽  
P. Guru Prakash
Keyword(s):  
Moisture Absorption ◽  
Spectroscopic Studies ◽  
Stability Studies ◽  
Cyclodextrin Complex ◽  
In Vivo Evaluation ◽  
Folding Endurance ◽  
Site Of Action ◽  
Permeability Enhancer

The main purpose of the present study was to develop ocuserts of Fluconazole -CD (beta-cyclodextrin) complex and to evaluate both in vitro and in vivo. Fluconazole was made complex with -CD, and the release rate was controlled by HPMC K4M and ethyl cellulose polymers using dibutyl Phthalate as permeability enhancer. Drug-polymer interactions were studied by Fourier transform infrared spectroscopic studies. The formulated ocuserts were tested for physicochemical parameters of in vitro release and in vivo permeation in rabbits. The optimized formulations (F-5 and F-8) were subjected to stability studies. The formulated ocuserts were found to have good physical characters, thickness, diameter, uniformity in weight, folding endurance, less moisture absorption, and controlled release of drug both in vitro and in vivo. The optimized formulations retained their characteristics even after stability studies. The study clearly showed that this technique was an effective way of formulating ocuserts for retaining the drug concentration at the intended site of action for a sufficient period of time and to elicit the desired pharmacological response.

Preparation, characterizations and evaluation of antifungal activity of eugenol-linalool emulgel against anthrophilic dermatophytic trichophyton rubrum

2021 ◽  
pp. 1-15
Author(s):  
Abdullah Akram ◽  
Muhammad Khalid Khan ◽  
Barkat Ali Khan
Keyword(s):  
Antifungal Activity ◽  
Skin Infection ◽  
Trichophyton Rubrum ◽  
Sem Analysis ◽  
Antifungal Drugs ◽  
In Vivo Studies ◽  
Stability Studies ◽  
Antifungal Activities

Trichophyton rubrum (T. Rubrum) is responsible for chronic cases of dermatophytosis which have high rates of resistance to antifungal drugs worldwide. The aim of this study was to formulate an emulgel of Eugenol-Linalool for the treatment of T. Rubrum infections. The emulgel was prepared by slow emulsification method and characterized for physical examination, pH analysis, swelling index, stability studies, spreading coefficient, SEM analysis, thermal analysis and PXRD studies. In-vitro antifungal activities were performed by growing T. rubrum on specialized media in petri dishes. In-vivo antifungal activity was performed in rabbits by inducing the skin infection by application of fungal strain. Results indicated that the emulgel formulation is highly stable and the physical properties of the emulgel remained quite feasible. No deterioration was observed in the formulation and the pH remained the same as the pH of skin. The viscosity and spreadability of the emulgel remained highly compatible. The results of in vitro and in vivo studies indicated that the Eugenol and Linalool both inhibited the growth of T. rubrum. Eugenol was more effective in inhibition of zone (38±0.01 mm) of T. rubrum as compared to Linalool (32.9±0.03 mm). Similarly it was observed that when the combination of both Linalool and Eugenol was used, the growth of T. rubrum (42±0.01 mm) was significantly (P <  0.05) inhibited. It is hence concluded that the emulgel containing Eugenol and Linalool possess strong in vitro and in vivo antifungal activities against the commercial strains of anthrophilic dermophytic T. Rubrum.

scholarly journals DEVELOPMENT AND CHARACTERIZATION OF TRANSDERMAL DELIVERY SYSTEM OF DOXAZOSIN MESYLATE

2019 ◽  
Vol 11 (1) ◽  
pp. 43 ◽  
Author(s):  
Madhur Kulkarni ◽  
Vishakha Hastak ◽  
Supriya Jadhav
Keyword(s):  
Delivery System ◽  
Transdermal Delivery ◽  
Skin Irritation ◽  
Stability Studies ◽  
Accelerated Stability ◽  
In Vitro Permeation ◽  
Folding Endurance ◽  
Transdermal Delivery System

Objective: The study involved development of transdermal delivery system (TDDS) of doxazosinmesylate (doxa) to achieve effective systemic delivery of the drug.Methods: TDDS of doxa was prepared using hydroxypropyl methyl cellulose (HPMC) K100LV and polyvinyl pyrrolidone (PVP) K30 in 3:1 ratio solvent casting method. The formulation was evaluated for folding endurance, moisture uptake, pH, drug content and in vitro permeation. Various permeation enhancers were incorporated at 5% w/w concentration into the patch formulationto study their impact on the drug permeation. The TDDS made with Transcutol® as an enhancer was subjected to accelerated stability studies and in vivo skin irritation studies.Results: The developed TDDS showed folding endurance of 170, moisture uptakeof 15.7%, pH of 6.3, and drug content of 99±1.1% and 66% in vitro permeation of doxa over 24h. The effect of various enhancers expressed in terms of average flux can be summarized as Transcutol® (10.6±2.1 µg/cm2h)>dimethyl sulfoxide(10.17±1.2 µg/cm2h)>benzyl alcohol (9.55±1.3 µg/cm2h)>no enhancer (8.86±1.1 µg/cm2h)>dimethyl isosorbide (8.21±1.5 µg/cm2h)>Isostearic acid (7.82±1.4 µg/cm2h)>propylene carbonate (7.67±1.4 µg/cm2h)>oleic acid (7.12 µg±0.8/cm2h). The formulation was found to be stable during the accelerated stability studies. In vivo studies indicated absence of skin irritation effect the TDDS containing Transcutol®.Conclusion: TDDS of doxa comprising HPMC K100LV and PVPK30 in the ratio of 3:1 and 5% Transcutol® could serve as a potential TDDS in the treatment of benign prostatic hyperplasia (BPH) and hypertension.

scholarly journals Utilization of Poloxamer as Well as Combinations with Other Polymers as Base in Ophthalmic in Situ Gel Dosage Form

2020 ◽  
Vol 10 (01) ◽  
pp. 101-105
Author(s):  
Insan Sunan Kurniawansyah ◽  
Taofik Rusdiana ◽  
Iyan Sopyan ◽  
Anas Subarnas ◽  
Habibah A. Wahab
Keyword(s):  
Drug Release ◽  
Dosage Form ◽  
Stability Studies ◽  
In Vitro Drug Release ◽  
In Situ Gel ◽  
Rabbit Eye ◽  
Release Drug

The aim of this review was to find out which formulation were good for making in-situ gels using a combination of poloxamer and other bases. Formulation was characterized for appearance and homogeneity, pH and gelation studies, viscosity measurements, in vitro drug release, drug content, and stability studies. In vivo rabbit, eye irritation tests were conducted to evaluate the irritation of the in-situ gel delivery system; in addition, osmolality testing, sterility test, and isotonicity evaluation were also carried out. The results have shown that in-situ gel solution can increase residence time and also maintain the mechanism of drug release.

Very stable 188Re-S4 chelates for labelling biomolecules

2007 ◽  
Vol 46 (05) ◽  
pp. 181-184 ◽  
Author(s):  
C. Jentsche ◽  
R. Bergmann ◽  
H.-J. Pietzsch ◽  
G. Wunderlich ◽  
J. Kotzerke ◽  
...  
Keyword(s):  
Ascorbic Acid ◽  
Specific Activity ◽  
Direct Reduction ◽  
High Specific Activity ◽  
Amine Group ◽  
Stability Studies ◽  
Therapeutic Application ◽  
Carboxylic Groups

SummaryAim: The preparation and stability of a new 188Re-S4-complex [S4 = (1-aza-18-crown-6)(O)C-C(SH)-C(SH)- C(O)NH-(CH2)3-NH-(CH2)3-NHC(O)-C(SH)-C(SH)- C(O)(1-aza-18-crown-6] was studied at therapeutic relevant radioactive concentrations. The results were compared with 188Re-MAG3 (MAG3: mercaptoacetyltriglycine) and 188Re-DMSA preparations (DMSA: dimercaptosuccinic acid) performed with the same highly concentrated [188Re]perrhenate solution (12-15 GBq/ml). Methods: The 188Re complexes were prepared by direct reduction of perrhenate (188Re-S4-complex) as well as via the 188Re- EDTA precursor complex (188Re-MAG3, 188Re-DMSA). The preparations were stabilised with 15 mg of ascorbic acid and analysed after 1, 2, and 24 hours by TLC and HPLC. Additionally, in vitro and in vivo stability studies were performed with the purified complexes. Results: After stabilisation with 15 mg of ascorbic acid, all of the complexes were nearly stable under nitrogen for hours, and only 2–8 % of perrhenate was observed after 24 h. In contrast, only the 188Re-S4 complex was completely stable in vitro and in all investigated in vivo samples after separation of ligand excess and reducing agent by HPLC. Conclusion: The bridging amine group or free carboxylic groups of the S4-ligand framework make available reactive positions for coupling biomolecules to the chelate. Thus it appears that the new 188Re-S4 complexes offer the possibility of stable and high specific activity labelling of biomolecules for therapeutic application.

scholarly journals Degradomics-Based Analysis of Tetanus Toxoids as a Quality Control Assay

Vaccines ◽  
2020 ◽  
Vol 8 (4) ◽  
pp. 712
Author(s):  
Thomas J. M. Michiels ◽  
Wichard Tilstra ◽  
Martin R. J. Hamzink ◽  
Justin W. de Ridder ◽  
Maarten Danial ◽  
...  
Keyword(s):  
Drug Product ◽  
Absolute Quantification ◽  
In Vitro Assays ◽  
Cathepsin S ◽  
Stability Studies ◽  
Liquid Chromatography Mass Spectrometry ◽  
Batch Release ◽  
Antigen Presenting

Currently, batch release of toxoid vaccines, such as diphtheria and tetanus toxoid, requires animal tests to confirm safety and immunogenicity. Efforts are being made to replace these tests with in vitro assays in a consistency approach. Limitations of current in vitro assays include the need for reference antigens and most are only applicable to drug substance, not to the aluminum adjuvant-containing and often multivalent drug product. To overcome these issues, a new assay was developed based on mimicking the proteolytic degradation processes in antigen-presenting cells with recombinant cathepsin S, followed by absolute quantification of the formed peptides by liquid chromatography-mass spectrometry. Temperature-exposed tetanus toxoids from several manufacturers were used as aberrant samples and could easily be distinguished from the untreated controls by using the newly developed degradomics assay. Consistency of various batches of a single manufacturer could also be determined. Moreover, the assay was shown to be applicable to Al(OH)3 and AlPO4-adsorbed tetanus toxoids. Overall, the assay shows potential for use in both stability studies and as an alternative for in vivo potency studies by showing batch-to-batch consistency of bulk toxoids as well as for aluminum-containing vaccines.

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