Development of Moxifloxacin Hydrochloride Thermoreversible Ocular Delivery System for the Treatment of Conjunctivitis

2020 ◽  
Vol 10 (7) ◽  
pp. 1010-1014
Author(s):  
Jing Huang ◽  
Yong Cui ◽  
Chunting Sun ◽  
Xinyan Liu
Keyword(s):  
Drug Release ◽  
Delivery System ◽  
Retention Time ◽  
Poloxamer 407 ◽  
Contact Site ◽  
Common Disorder ◽  
Sustained Action ◽  
Gelling Time ◽  
Ocular Delivery System

The present investigation deals with formulation and development of novel ophthalmic in situ gel formulation of Moxifloxacin in order to treat common disorder of conjunctivitis. The formulation contains combination of two polymers like Poloxamer 4–7 and chitosan both help in sustaining and increasing the drug release as well as retention time of drug at contact site. Thus developed formulation was evaluated for various parameters. The moxifloxacin in situ gel was found to be clear with ph in range of 6.8–7.0. The gelling time was also found to be quick with prolong retention up to 8 hrs. The optimized batch showed maximum release of 99.98% and was found to have sustained action when compared to marketed ophthalmic eye drop formulation. The formulation of Ophthalmic Thermosensitive in situ gel for Moxifloxacin was successfully prepared using Polymer combination of Poloxamer 407 and chitosan and found effective in the treatment of Conjunctivitis.

In Vitro and In Vivo Drug Release from a Novel In Situ Forming Drug Delivery System

2007 ◽  
Vol 25 (6) ◽  
pp. 1347-1354 ◽  
Author(s):  
Heiko Kranz ◽  
Erol Yilmaz ◽  
Gayle A. Brazeau ◽  
Roland Bodmeier
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
In Situ Forming

DEVELOPMENT AND EVALUATION OF NANOPARTICULATE BASED IN-SITU GELLING SYSTEM FOR NASAL DRUG DELIVERY OF AN ANTI-EPILEPTIC DRUG

INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (09) ◽  
pp. 83-85
Author(s):  
A Ambavkar ◽  
◽  
N. Desai
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Entrapment Efficiency ◽  
Poloxamer 407 ◽  
Nasal Drug Delivery ◽  
Anti Epileptic Drug ◽  
Nanolipid Carriers ◽  
In Situ Nasal Gel

The objective of the study was to develop and evaluate nanolipid carriers based in situ gel of Carbamazepine, for brain delivery through intranasal route. The non – invasive nasal route can provide rapid delivery of drugs directly to the central nervous system by bypassing the blood brain barrier. The nanolipid carriers of carbamazepine as in situ nasal gel can prolong the drug release for control of repetitive seizures and were prepared by Phase Inversion Temperature technique. The retention of the carriers in the nasal cavity was improved by using Poloxamer 407 as thermoresponsive and Carbopol 974P as mucoadhesive gelling polymers, respectively. The developed gel was evaluated for particle size, polydispersity index, zeta potential, morphology, entrapment efficiency, mucoadhesive and thermoresponsive behaviour, in vitro drug release, ex vivo permeation and nasociliotoxicity. The gel showed sustained release over prolonged periods and was found to be non-toxic to the sheep nasal mucosa.

scholarly journals Injectable Thermo-Sensitive Chitosan Hydrogel Containing CPT-11-Loaded EGFR-Targeted Graphene Oxide and SLP2 shRNA for Localized Drug/Gene Delivery in Glioblastoma Therapy

2020 ◽  
Vol 21 (19) ◽  
pp. 7111 ◽  
Author(s):  
Yu-Jen Lu ◽  
Yu-Hsiang Lan ◽  
Chi-Cheng Chuang ◽  
Wan-Ting Lu ◽  
Li-Yang Chan ◽  
...  
Keyword(s):  
Graphene Oxide ◽  
Gene Delivery ◽  
Drug Release ◽  
Delivery System ◽  
Targeted Delivery ◽  
Drug Formulation ◽  
Treatment Modalities ◽  
Gene Delivery System ◽  
Optimal Drug

In this study, we aimed to develop a multifunctional drug/gene delivery system for the treatment of glioblastoma multiforme by combining the ligand-mediated active targeting and the pH-triggered drug release features of graphene oxide (GO). Toward this end, we load irinotecan (CPT-11) to cetuximab (CET)-conjugated GO (GO-CET/CPT11) for pH-responsive drug release after endocytosis by epidermal growth factor receptor (EGFR) over-expressed U87 human glioblastoma cells. The ultimate injectable drug/gene delivery system was designed by co-entrapping stomatin-like protein 2 (SLP2) short hairpin RNA (shRNA) and GO-CET/CPT11 in thermosensitive chitosan-g-poly(N-isopropylacrylamide) (CPN) polymer solution, which offers a hydrogel depot for localized, sustained delivery of the therapeutics after the in situ formation of CPN@GO-CET/CPT11@shRNA hydrogel. An optimal drug formulation was achieved by considering both the loading efficiency and loading content of CPT-11 on GO-CET. A sustained and controlled release behavior was found for CPT-11 and shRNA from CPN hydrogel. Confocal microscopy analysis confirmed the intracellular trafficking for the targeted delivery of CPT-11 through interactions of CET with EGFR on the U87 cell surface. The efficient transfection of U87 using SLP2 shRNA was achieved using CPN as a delivery milieu, possibly by the formation of shRNA/CPN polyplex after hydrogel degradation. In vitro cell culture experiments confirmed cell apoptosis induced by CPT-11 released from acid organelles in the cytoplasm by flow cytometry, as well as reduced SLP2 protein expression and inhibited cell migration due to gene silencing. Finally, in vivo therapeutic efficacy was demonstrated using the xenograft of U87 tumor-bearing nude mice through non-invasive intratumoral delivery of CPN@GO-CET/CPT11@shRNA by injection. Overall, we have demonstrated the novelty of this thermosensitive hydrogel to be an excellent depot for the co-delivery of anticancer drugs and siRNA. The in situ forming hydrogel will not only provide extended drug release but also combine the advantages offered by the chitosan-based copolymer structure for siRNA delivery to broaden treatment modalities in cancer therapy.

Benzoyl Peroxide In Situ Forming Antimicrobial Gel for Periodontitis Treatment

2013 ◽  
Vol 545 ◽  
pp. 63-68 ◽  
Author(s):  
Jongjan Mahadlek ◽  
Juree Charoenteeraboon ◽  
Thawatchai Phaechamud
Keyword(s):  
Drug Delivery ◽  
Antimicrobial Activity ◽  
Drug Release ◽  
Delivery System ◽  
Periodontal Pocket ◽  
Peppermint Oil ◽  
In Situ Gel ◽  
In Situ Forming ◽  
In Situ Forming Gel

Periodontitis is an inflammatory disease of the supporting structures of the tooth caused by bacterial infection which can result in tooth loss. The local intra-pocket drug delivery system was interesting and highly effective for periodontitis treatment. In situ forming gel system is the polymeric solution which could transform into gel for localizing and sustaining the drug release at desired site. This system has been recommended as one of suitable delivery system for this purpose. Benzoyl peroxide (BPO) in situ forming gels were developed using Eudragit RS as polymer dispersed in N-methyl-pyrrolidone (NMP). Peppermint oil and polyethylene glycol 1500 were also incorporated as the excipients. The prepared systems were evaluated for rheology, syringeability (using texture analyzers), in situ gel formation (after injection into PBS pH 6.8), antimicrobial activity (against Streptococcus mutans with agar diffusion) and drug release (with dialysis method in PBS pH 6.8 at 50 rpm, 37 °C). The viscosity and syringeability of the prepared systems was increased as the amount of BPO, peppermint oil or PEG 1500 was increased. All prepared gels showed the Newtonian flow which the viscosity was decreased as the temperature was increased. All prepared gels comprising peppermint oil and PEG 1500 could form in situ gel in used medium which the pH was close to the environment pH of periodontal pocket. The inhibition zone against Streptococcus mutans of the prepared system was significantly decreased when the peppermint oil and PEG 1500 was incorporated owing to the higher viscous environment and thereafter retardation of drug diffusion was evident. This effect could prolong the drug release. From drug release test, all prepared gels could sustain the BPO release for at least 96 hrs. Release kinetic obtained from curve fitting with various release equations using least square fit technique indicated that the release patterns were as Higuchi’s model therefore the release of BPO was performed with diffusion control. This developed BPO in situ forming gel presented its ability as the controlled drug delivery system for localized antimicrobial activity at periodontal pocket.

scholarly journals Optimization of ThermoreversibleIn SituNasal Gel of Timolol Maleate

Scientifica ◽  
2016 ◽  
Vol 2016 ◽  
pp. 1-11 ◽  
Author(s):  
Swati Jagdale ◽  
Nirupama Shewale ◽  
Bhanudas S. Kuchekar
Keyword(s):  
Drug Release ◽  
Factorial Design ◽  
Ex Vivo ◽  
Nasal Delivery ◽  
Poloxamer 407 ◽  
Timolol Maleate ◽  
First Pass Metabolism ◽  
First Pass ◽  
Pass Metabolism

Nasal route had shown better systemic bioavailability due to its large surface area, porous endothelial membrane, high total blood flow, and avoidance of first-pass metabolism. Timolol maleate is a beta blocker used primarily in the treatment of hypertension. Drug undergoes extensive hepatic first-pass metabolism (80%). The drug has half-life of 4 hrs. Oral bioavailability of timolol maleate is 61%. The aim of the present study was to optimize controlled releasein situnasal delivery for timolol maleate. HPMC and Poloxamer 407 were selected as polymer in formulation of thermoreversiblein situnasal gel. Optimization was carried out using 32factorial design. It was observed that formulations f1 and f4 revealed the highest % drug release, that is, 93.57% and 91.66%, respectively. Factorial design study indicated that the drug release and viscosity were most significant dependent factors.Ex vivodiffusion study through nasal mucosa indicated 67.26 ± 2.10% and 61.07 ± 2.49% drug release for f1 and f4 formulations. f1 was the optimized batch. This batch thus can act as a potential nasal delivery with enhanced bioavailability for the drug.

Preparation of Liquid Oral Mucoadhesive Gastro-retentive System of Nimodipine

2019 ◽  
Vol 16 (9) ◽  
pp. 862-871 ◽  
Author(s):  
Mai Mamdouh ◽  
Ahmed Donia ◽  
Ebtessam Essa ◽  
Gamal El Maghraby
Keyword(s):  
Critical Care ◽  
Controlled Release ◽  
Drug Release ◽  
Release Rate ◽  
Poloxamer 407 ◽  
Liquid Form ◽  
Drug Release Rate ◽  
Alginate Concentration ◽  
Gastro Retentive

Background: Nimodipine is a calcium channel blocker frequently used in critical care settings. It is mainly absorbed in the upper gastrointestinal tract. Accordingly, the development of gastroretentive formulation will be beneficial. The benefit would be maximized for critical care patients if the developed system was in liquid form to facilitate the administration through nasogastric tubing. Objective: Development of gastro-retentive liquid oral controlled release formulation of nimodipine through in situ gellation. Methods: Nimodipine dissolution was improved by solid dispersion (SD) using poloxamer 407. Sodium alginate solutions (1, 1.5 and 2%w/v) were loaded with the optimized SD microparticles. Carboxymethylcellulose was added to modulate the release and to augment mucoadhesion power. All in situ gelling alginate solutions were characterized regarding viscosity, gelling capacity and drug release. SD microparticles showed considerable improvement in nimodipine dissolution. Results: All alginate systems were pourable. Increasing alginate concentration increased the gelling capacity and reduced drug release rate. The addition of carboxymethylcellulose produced greater control over drug release rate. X-ray radiography showed successful stomach-retention over 8 hours in rabbits, which correlates with the controlled release pattern of the developed systems. Conclusion: The study provides the formulator with a range of gastroretentive controlled release formulations of nimodipine while maintaining the convenience of administration through nasogastric tubing with the potential for enhanced bioavailability.

A lutein ocular delivery system based on nanovesicles entrapped in an in situ forming gel

2013 ◽  
Vol 172 (1) ◽  
pp. e61
Author(s):  
Qingxiang Guan ◽  
Jingwen Lu ◽  
Tianmu Lin ◽  
Chen Chen ◽  
Chen Qian ◽  
...  
Keyword(s):  
Delivery System ◽  
Ocular Delivery ◽  
In Situ Forming ◽  
In Situ Forming Gel ◽  
Ocular Delivery System

scholarly journals Formulation and Evaluation of Sustained Release Sumatriptan Mucoadhesive Intranasal in-Situ Gel

2019 ◽  
Vol 28 (2) ◽  
pp. 95-104
Author(s):  
Hussein K. Alkufi ◽  
Hanan J. Kassab
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Poloxamer 407 ◽  
Gelation Temperature ◽  
In Vitro Drug Release ◽  
In Situ Gel ◽  
Ex Vivo Permeation ◽  
Ex Vivo Permeation Study

     Objective: The purpose of this study to develop and optimize nasal mucoadhesive in situ gel IG of sumatriptan ST (serotonin agonist) to enhance nasal residence time for migraine management.      Method: Cold method was used to prepare ST nasal in-situ gel, using thermosensitive polymers (poloxamer 407  and/or poloxamer 188) with a mucoadhesive polymer (hyaluronic acid HA) which were examined for gelation temperature and gelation time, pH, drug content, gel strength, spreadability, mucoadhesive force determination, viscosity,  in-vitro drug release, and the selected formula was subjected to ex-vivo permeation study and histological evaluation of the sheep mucosal tissue after application.     Results: The results showed that the formula IG7 prepared from poloxamer 407(19%), poloxamer188 (4%) and HA (0.5%)   had an optimum gelation temperature (32.66±1.52°C), gel  strength (43.66± 1.52 sec),  mucoadhesive force (8067.93± 746.45dyne\cm2), in-vitro drug release (95.98%) over 6hr, ex-vivo permeation study release (89.6%)  during the 6 h. study with no  histological or pathological change in the nasal sheep tissue.     Conclusion: The ease of administration via a nasal drop of ST coupled with less frequent administration and prolong drug release, will enhance patient compliance.

Development of In Situ Gel for Oral Application

2014 ◽  
Vol 1060 ◽  
pp. 66-69
Author(s):  
Suwannee Panomsuk ◽  
Pimchanok Nakprasong ◽  
Suthi On Tanpichai ◽  
Sasithorn Chin-Aramrungruang
Keyword(s):  
Drug Release ◽  
Buccal Mucosa ◽  
Sol Gel ◽  
Gel Strength ◽  
Medical Product ◽  
Poloxamer 407 ◽  
In Situ Gel ◽  
Model Drug ◽  
Gel Temperature

In situ gel, a new concept of medical product for oral applications was developed using Poloxamer 407 (P) and Carbopol 934 (C) which are thermo-and pH-sensitive sol-gel polymers, respectively. The formulations were evaluated for the physical appearance, pH, viscosity, sol-gel temperature, gel strength and buccal mucoadhesive (adhesion to porcine buccal mucosa). Benzalkonium chloride (BzCl) 0.1% w/v was added in the suitable formulations as a model drug. Formulations containing 20% P (pH = 7.1) and 20% P + 0.6% C (pH = 5.0) showed good physical appearances which turned to gels in buccal conditions. Their mucoadhesive force to porcine buccal mucosa were higher than formulations containing 10 and 15 % P(p<0.05). The present of 0.6 % C in the formulation did not affect gel strength but tended to increase mucoadhesive properties. The release of BzCl from the formulations was performed using Franz diffusion cell at 37°C for 1 hour. There were no different in drug release from both formulations(p<0.05), the amount of drug release was 11.7% ± 4.4 and 10.9% ± 0.8, respectively. In conclusion, formulation containing 20% P and 0.6% C has revealed the most suitable properties as in situ gel for buccal mucosa applications, the release of BzCl was 10.9% ± 0.8 within 1 hour.

Sign in / Sign up

Export Citation Format

Share Document