scholarly journals Formulation Development and Characterisation of Gemifloxacin Mesylate and Loteprednol Etabonate Ophthalmic Ocuserts

2020 ◽  
Vol 11 (2) ◽  
pp. 2549-2557
Author(s):  
Swati Mayur Keny ◽  
Ketan Shah

Gemifloxacin Mesylate is a fluoroquinolone antibacterial drug preferably used in the treatment of bacterial conjunctivitis. The addition of Loteprednol Etabonate enhances the anti-inflammatory activity of the developed formulation. The objective of the present work was to develop ocular inserts of Gemifloxacin Mesylate with Loteprednol Etabonate and thereby evaluate its potential as a sustained ocular delivery system. Poor bioavailability and poor therapeutic responses are associated with conventional ophthalmic solutions due to many pre-corneal constraints. These constrain trigger the researcher's mind to formulate a controlled and sustained drug delivery system. Ocular inserts based on the solvent cast technique were formulated and characterized by in vitro drug release studies using a flow-through apparatus that simulated the eye conditions. Compatibility of Gemifloxacin Mesylate, Loteprednol Etabonate, polymer, and excipients was checked based on preformulation studies. Different combinations of Gemifloxacin Mesylate, Loteprednol Etabonate, Carbopol 974, 98 981, PEG 400, and glycerine were formulated by the solvent cast method and evaluated. Clarity, smoothness, surface pH, drug content, and in-vitro drug release study were the various parameters evaluated on the formulated ocusert. Formula GLE 74 fulfilled the needs of all organoleptic parameters and also the in-vitro release study. Based on in vitro correlation stability studies, it was concluded that this ocular inserts formulation could be a promising controlled release formulation.

Author(s):  
Nani Tadhi ◽  
Himansu Chopra ◽  
Gyanendra Kumar Sharma

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.


Author(s):  
Naga sai divya K ◽  
T Malyadri ◽  
Ch.saibabu

The purpose of the present study was to develop and optimize the emulgel system for Luliconazole using different types of gelling agents: HPMCK15M, Carbopol 940, and Xanthan Gum. The prepared emulgels were evaluated in terms of appearance, pH, spreadability, viscosity, drug content, and in-vitro drug release. In-vitro release study demonstrated diffusion-controlled release of Luliconazole from formulation up to 12 hours. The drug release profile exhibited zero-order kinetics. All the prepared emulgels showed acceptable physical properties concerning color, homogeneity, consistency, spreadability, and higher drug release. In the case of all evaluation parameters, carbopol based formulation showed better properties so, as a general conclusion, it was suggested that the Luliconazole emulgel formulation prepared with carbopol (F6) was the formula of choice.


2019 ◽  
Vol 9 (4-A) ◽  
pp. 72-78
Author(s):  
Prashant L Pingale ◽  
R. P. Ravindra

Bioenhancers are the ‘bioavailability enhancers’; they do not show any therapeutic effect, but when used in combination enhances the activity of drug molecule. In a cited research paper, the effect of various species of piper used as bioenhancer singly and in combination in an equal ratio. The methods used for preparation of microspheres are Complex Coacervation and Modified Emulsion Method. The prepared microspheres were evaluated for various parameters like in-vitro release, drug entrapment efficiency, percent bioadhesion, permeability study using intestinal sac method. The in-vitro drug release of drugs from formulations where Piper nigrum was used as bioenhancers was found to be about 66-70% in 12 hrs. when used singly. When bioenhancers used in combination the in-vitro drug release of drugs was increased up to 85-90% for combination of Piper album and Piper longum in an equal proportion, the same was about 35-40% in case of formulations where no bioenhancers was used. The microspheres found to be less than 130 micron in size. The DEE was found to be in the range of 27-67%. The bioadhesion of the microsphere were found to be 20-76% (increased in formulations where bioenhancers incorporated). The in- vitro release study by USP paddle apparatus, the important results from in-vitro release study relates to the very significant enhancement in drug release, due to presence of bioenhancers. Keywords: Microspheres, Bioenhancer, Piper nigrum, Piper album, Piper longum, Pyrazinamide, Ethambutol


2019 ◽  
Vol 70 (7) ◽  
pp. 2347-2349
Author(s):  
Ramona-Daniela Pavaloiu ◽  
Fawzia Sha At ◽  
Corina Bubueanu ◽  
Cristina Hlevca ◽  
Gheorghe Nechifor

The aim of this paper was the design and evaluation of delivery system for Armoracia rusticana leaves extract with the purpose to use such systems in food or cosmetic field. Liposomes loaded with Armoracia rusticana were prepared by film hydration method and presented good entrapment efficiency, nano-sizes ([150 nm), low polydispersity index and good stability over 90 days at 4oC. In vitro drug release study showed the ability of liposomes to provide slow release of extract with reduced burst effect compared to free extract. These promising results suggest that liposomes could be exploited as carriers for herbal ingredients.


2021 ◽  
Vol 10 (2) ◽  
pp. 56-60
Author(s):  
J Adlin Jino Nesalin ◽  
Shafiya Khanum

The main objective of this research is to evaluate a new approach for the preparation of bio adhesive microparticles and to design an innovative vaginal delivery system for curcumin which is able to enhance the drug anticancer activity. Curcumin encapsulated microspheres were prepared by solvent evaporation method. The microspheres were found to be discrete, spherical with free-flowing properties and evaluated for particle size analysis, shape (scanning electron microscopy), drug encapsulation efficiency, FTIR, DSC studies and in vitro release performance. The best selected microsphere formulation (F2, containing drug: polymer ratio 1:2) was incorporated into gels with a bio adhesive polymer. The microencapsulated vaginal gels were evaluated for pH, spreadability, extrudability, viscosity, in vitro drug release, drug release kinetics, bio adhesion test, accelerated stability of selected gel formulation. In vitro drug release rate for selected microencapsulated bio adhesive vaginal gel (FS3 gel, containing 1 % w/w of drug loaded microspheres and 0.6 % w/w of Carbopol 934) was found to sustain curcumin over 12h. The results were then compared statistically and obtained a satisfactory correlation. Thus, in conclusion preparation protocol of microencapsulated vaginal gel study may be adopted for a successful development of newer drug delivery system of other drugs for administration to vagina.


2020 ◽  
Vol 10 (5) ◽  
pp. 175-181
Author(s):  
Yogita Sahu ◽  
Sourabh Jain ◽  
Karunakar Shukla

The purpose of research work was to develop and optimize mucoadhesive microspheres of Ziprasidone hydrochloride for nasal delivery with the aim to enhance the residence time and improve therapeutic efficacy. Mucoadhesive drug delivery systems are those that provide intimate contact of the drug with the mucosa for an extended period of time. In our present work, mucoadhesive chitosan microspheres were prepared by emulsification method using liquid paraffin as external phase. Ten different formulations were developed. Results show that as the concentration of polymer increases it affects the particle size, production yield, encapsulation efficiency, swelling index, in-vitro mucoadhesion and in-vitro drug release of mucoadhesive microspheres. The in vitro mucoadhesion of microspheres was investigated using freshly isolated goat nasal mucosa. The mucoadhesion for M0, M1, M2, and M9 was tested. The mucoadhesion property was satisfactory. The M2 exhibited lowest mucoadhesion of 68.9%, and M0 displayed highest mucoadhesion of 87.5%. The In Vitro release studies it revealed that 84.1% of drug release from formulation M1 at 7hrs. The 50% of the drug was released from the formulation M2 and 70.67% from formulation M9.This formulations were further used for SEM for particles size analysis, mucoadhesion test and in-vitro drug release. The In-vitro % drug release data suggest that the maximum and sustained drug release was obtained for formulation M1.The present study showed that Ziprasidone hydrochloride chitosan microspheres can deliver intanasally which can improve the therapeutic outcome for the Epileptic seizure. Keywords: Ziprasidone hydrochloride, Mucoadhesive microspheres, Nasal drug delivery, Drug Entrapment efficiency.


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