HPTLC analysis of tamoxifen citrate in drug-release media during development of an in-situ-cross-linking delivery system

Peptic ulcer, it is the most common type of stomach disease, according to the American Gastroenterology Association. “We know that ulcers occur because there has been a disruption in the balance of factors that injure the digestive tract and those factors that protect it from injury,” The present investigation deal with the formulation, optimization and evaluation of sodium alginate based in situ gel of ranitidine hydrochloride (R-HCl) in ulcer treatment. The in-situ formulation are homogenous liquid when administration orally and become gel at the contact site. The evaluation of the formulation is dependent upon accurate results obtained by analytical method used during the study. Accurate results require the use of standard and a calibration procedure. Hence, standard plots of Ranitidine hydrochloride were prepared in (0.1N HCL, pH 1.2) solutions. Two, sodium alginate and calcium carbonate used as a polymer and cross-linking agent respectively in the formulation of in-situ gel. From the IR studies it may be concluded that the drug and carriers used undergo physical interaction there is no chemical change, and thus the gelling agent, cross-linking agent and other excipient is suitable for formulation of in-situ gel of ranitidine hydrochloride. Indicate that the formulation, DKF9 which was prepared by the Sodium alginate (2 gm) with Ranitidine Hydrochloride showed minimum drug release (sustained drug release) after 8 hrs. It can be concluded that the In-situ gel was beneficial for delivering the drug which needs sustained release to achieve the slow action. Keywords: In-situ gel, Peptic Ulcer, Ranitidine Hydrochloride (R-HCl), Sodium alginate.

Download Full-text

Injectable in situ cross-linking hyaluronic acid/carboxymethyl cellulose based hydrogels for drug release

Journal of Biomaterials Science Polymer Edition ◽

10.1080/09205063.2018.1481005 ◽

2018 ◽

Vol 29 (13) ◽

pp. 1643-1655 ◽

Cited By ~ 7

Author(s):

Shuang Deng ◽

Xian Li ◽

Wangkai Yang ◽

Kewen He ◽

Xu Ye

Keyword(s):

Hyaluronic Acid ◽

Drug Release ◽

Carboxymethyl Cellulose ◽

Cross Linking

Download Full-text

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

International Journal of Molecular Sciences ◽

10.3390/ijms21197111 ◽

2020 ◽

Vol 21 (19) ◽

pp. 7111 ◽

Cited By ~ 2

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.

Download Full-text

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

Journal of Biomaterials and Tissue Engineering ◽

10.1166/jbt.2020.2365 ◽

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.

Download Full-text

Benzoyl Peroxide In Situ Forming Antimicrobial Gel for Periodontitis Treatment

Key Engineering Materials ◽

10.4028/www.scientific.net/kem.545.63 ◽

2013 ◽

Vol 545 ◽

pp. 63-68 ◽

Cited By ~ 8

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.

Download Full-text