Sustained vaginal delivery of in situ gel containing Voriconazole nanostructured lipid carrier: formulation, in vitro and ex vivo evaluation

2022 ◽  
pp. 1-13
Author(s):  
Ruchika M. Bondre ◽  
Pranita S. Kanojiya ◽  
Rita N. Wadetwar ◽  
Priya S. Kangali
Keyword(s):  
Vaginal Delivery ◽  
Ex Vivo ◽  
Nanostructured Lipid Carrier ◽  
In Situ Gel

Preparation of levofloxacin loaded in situ gel for sustained ocular delivery: in vitro and ex vivo evaluations

2019 ◽  
Vol 46 (1) ◽  
pp. 50-56 ◽  
Author(s):  
Pooja Jain ◽  
Chandra Prakash Jaiswal ◽  
Mohd. Aamir Mirza ◽  
Md. Khalid Anwer ◽  
Zeenat Iqbal
Keyword(s):  
Ex Vivo ◽  
Ocular Delivery ◽  
In Situ Gel

Fabrication and Characterization of Ocular Phase Transition Systems for Blepharitis: A Novel Approach

2020 ◽  
Vol 10 (1) ◽  
pp. 24-37
Author(s):  
Deepali Verma ◽  
Shreya Kaul ◽  
Neha Jain ◽  
Upendra Nagaich
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Eye Drops ◽  
Stability Studies ◽  
In Vitro Drug Release ◽  
In Situ Gel ◽  
Drug Content ◽  
Erythromycin Estolate

Introduction: In the present research, erythromycin estolate loaded in-situ gel was formulated and evaluated for blepharitis in order to improve its therapeutic efficacy, precorneal residence time of the system and to enhance the ocular bioavailability. Material and Methods: The developed formulation was characterized by several parameters viz. FTIR, clarity, pH, gelation temperature, rheological studies, drug content, in vitro drug release studies, transcorneal permeation studies, bioadhesion studies, isotonicity and stability studies. Results: The optimized formulation exhibited non-fickian release diffusion with a sustained release of drug 82.76 ± 0.94% up to 8h and drug content 93.64%. Isotonicity revealed that the formulation was isotonic in nature and there was no shrinkage and busting of cells. Bioadhesion study was performed to check the adherence of the prepared in situ gel to the corneal surface for 4h. Ex vivo transcorneal permeation was observed to be significantly higher when compared with market eye drops. Histopathological studies were conducted to confirm the presence of normal ocular surface tissues by maintaining their morphological structures without causing damage to the tissues. The formulation was nonirritant as confirmed by the HET-CAM test. Stability studies and accelerated stability studies were conducted for 13 weeks and 26 weeks respectively and formulations were analyzed for the visual appearance, pH, viscosity, gelling capacity, drug content and in vitro drug release and results showed no change in the formulations. Conclusion: The formulation was therapeutically efficacious, sterile, stable and provided controlled release over a period of time. The developed system could be a viable alternative to conventional eye drops for treatment of various ocular diseases.

scholarly journals Thermosensitive Brinzolamide in situ Gel Nanoemulsions, in vitro and ex vivo Evaluation

2020 ◽  
Vol 11 (1) ◽  
pp. 7754-7764
Keyword(s):  
Carbonic Anhydrase ◽  
Ex Vivo ◽  
Physical Stability ◽  
Topical Administration ◽  
Physicochemical Characteristics ◽  
Spontaneous Emulsification ◽  
In Situ Gel ◽  
Physicochemical Features

Brinzolamide (BZ) is a carbonic anhydrase inhibitor with selectivity and affinity for the carbonic anhydrase type II isoenzyme that administrated topically as an ophthalmic suspension for reducing intraocular pressure. In this study, BZ in situ gel nanoemulsions (NEs) were developed and evaluated for transcorneal permeation via the bovine corneal membrane. The spontaneous emulsification method was employed to prepare BZ in situ gel NEs. Various physicochemical characteristics, including particle size, polydispersity index, pH, refractive index, and viscosity, were evaluated. Accelerated physical stability and in vitro drug release, as well as transcorneal permeation studies was performed by applying the Franz-type diffusion cells. Thermosensitive BZ in situ gel NEs with desired physicochemical features and sustained release profiles were designed in the current study. Optimized Formulations exhibited physical stability under different conditions. The transcorneal permeation of formulations was higher than that of suspension, especially for F3b formulation. According to the present in vitro and ex vivo evaluations, it is concluded that in situ gel NEs could be a topical administration of BZ as a suitable ocular drug 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.

An Ex Vivo Evaluation of Moxifloxacin Nanostructured Lipid Carrier Enriched In Situ Gel for Transcorneal Permeation on Goat Cornea

2019 ◽  
Vol 108 (9) ◽  
pp. 2905-2916 ◽  
Author(s):  
Shilpkala Gade ◽  
Krishna Kumar Patel ◽  
Chandan Gupta ◽  
Md. Meraj Anjum ◽  
Deepika Deepika ◽  
...  
Keyword(s):  
Ex Vivo ◽  
Nanostructured Lipid Carrier ◽  
In Situ Gel

scholarly journals Formulation development and characterization of in-situ gel of Rizatriptan Benzoate for intranasal delivery

2021 ◽  
Vol 11 (1-s) ◽  
pp. 1-6
Author(s):  
Jalaram H Thakkar ◽  
Shailesh T. Prajapati
Keyword(s):  
Ex Vivo ◽  
Gellan Gum ◽  
Brain Targeting ◽  
Great Promise ◽  
Formulation Development ◽  
In Situ Gel ◽  
Rizatriptan Benzoate ◽  
32 Factorial Design

The present investigation was aimed to formulate and characterize ion-activated in-situ gel loaded with Rizatriptan Benzoate (RIZ) for intranasal administration for brain targeting. The gel was further optimized for process and formulation parameters by using 32 factorial design. The optimized batch having the concentrations of gellan gum and HPMC E15 LV 33.83 mg and 9.6 mg respectively. Gel strength and mucoadhesive strength of the optimized formulation were found to be 32.54 sec and 2580.50 dynes/cm2 respectively. Moreover, improved in-vitro and ex-vivo release profile of in-situ gel were observed in comparison to drug solution. In a nutshell, the developed formulation holds a great promise in overcoming the limitation associated with currently marketed RIZ formulations and illustrates the potential use of ion-activated in-situ gel to administer the drug by nasal route for brain targeting. Keywords: In-situ gel, Rizatriptan benzoate, Ion-activated, Gellan gum, HPMC E15 LV, Brain delivery, Migraine

scholarly journals Formulation and Evaluation of Microemulsion Based in Situ Gel of Acyclovir for Vaginal Delivery

2020 ◽  
Vol 11 (4) ◽  
pp. 6336-6346
Author(s):  
Sanjeevani Shekhar Deshkar ◽  
Rutuja Prakash Bokare ◽  
Suhas Ashok Todmal
Keyword(s):  
Drug Release ◽  
Vaginal Delivery ◽  
Release Kinetics ◽  
Stability Study ◽  
Vaginal Tissue ◽  
Polyethylene Glycol 400 ◽  
In Situ Gel ◽  
Gelling Temperature

The purpose of the present study was to formulate and evaluate microemulsion based in situ gel of Acyclovir (ACV) for the vaginal delivery. The solubility of ACV in oils and surfactants and co-surfactant was evaluated to identify the components of the microemulsion. Microemulsion region was determined by using the pseudo-ternary phase diagrams for different formulations. Microemulsion formulation was prepared using Labrafil M1994C as oil phase, Cremophor RH40 as surfactant and Polyethylene glycol 400 and Transcutol P as co-surfactant and water. Microemulsion formulations were evaluated for pH, viscosity, conductivity and stability study. In situ gel of ACV, microemulsion was prepared using thermosensitive polymer, poloxamer.In situ gelwas characterized for viscosity, gelling temperature, the effect of dilution on gelling temperature, gelling ability, and in vitro drug release and release kinetics. The globule size of developed microemulsion was less than 100 nm with PDI in the range 0.307 to 0.641. The optimized microemulsion based in situ gel demonstrated shear thinning behaviour, the gelation temperature with and without dilution was in the range of 30-35ºC, and the drug release was sustained over eight hours. Mucoadhesive properties of microemulsion based in situ gel formulations were determined with a texture analyzer using a goat vaginal tissue, and the results indicated that the presence of microemulsion increased the mucoadhesion significantly. Microemulsion based in situ gel was successfully developed for vaginal delivery of Acyclovir.

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