INVESTIGATING THE EFFECT OF DIFFERENT GRADES AND CONCENTRATIONS OF PH‑SENSITIVE POLYMER ON PREPARATION AND CHARACTERIZATION OF LIDOCAINE HYDROCHLORIDE AS IN SITU GEL BUCCAL SPRAY

Objective: The present study was aimed to develop a pH-triggered in situ gel for local release of lidocaine hydrochloride (lidocaine HCL) in the buccal cavity to improve the anesthetic effect of this amino amide drug which has very high water solubility. The formulations were introduced to the oral cavity as a spray to improve compliance and for easier administration.Methods: In this work, two grades of carbopol (934 and 940)-based in situ gel spray were designed. The formulations containing lidocaine HCl 5% were prepared by mixing different concentrations of carbopol with xanthan gum. Eight formulations were investigated and evaluated for gelation capacity, spray angle, volume of solution delivered per each actuation, rheological properties, and release kinetic model. Similarity factor (f2) was used for the comparison of dissolution profiles.Results: The prepared formulations undergo gelation after it had been actuated to the buccal cavity as a spray solution. The results showed that, as the concentration of polymer was increased, the release of drug decreased and the viscosity increased for both grades. The spray angle and volume of solution delivered per each actuation varied according to the composition of each formulation. The in situ gel containing 0.3% carbopol 934 and 0.2% xanthan gum regarded as a better candidate which had a good gelation and release property compared to other formulations. Drug release from optimized in situ gel spray followed Korsmeyer–Peppas model and was mediated by Fickian diffusion mechanism.Conclusion: Lidocaine HCl-loaded pH-sensitive in situ gel was successfully developed using carbopol 934 as polymer to be applied to the buccal cavity as spray solution for more effective anesthetic effect and painless treatment.

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DEVELOPMENT AND CHARACTERIZATION OF IN SITU GEL OF XANTHAN GUM FOR OPHTHALMIC FORMULATION CONTAINING BRIMONIDINE TARTRATE

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2018.v11i7.25221 ◽

2018 ◽

Vol 11 (7) ◽

pp. 277 ◽

Cited By ~ 3

Author(s):

Vazir Ashfaq Ahmed ◽

Divakar Goli

Keyword(s):

Drug Release ◽

Xanthan Gum ◽

Gelation Time ◽

Gel Strength ◽

Eye Drops ◽

In Situ Gel ◽

23 Factorial Design ◽

Brimonidine Tartrate

Objective: The goal of this study was to develop and characterize an ion-activated in situ gel-forming brimonidine tartrate, solution eye drops containing xanthan gum as a mucoadhesive polymer.Method: Sol-gel formulation was prepared using gellan gum as an ion-activated gel-forming polymer, xanthan gum as mucoadhesive agent, and hydroxypropyl methyl cellulose (HPMC E50LV) as release retardant polymer. Phenylethyl alcohol is used as preservatives in borate buffer. The 23 factorial design was employed to optimize the formulation considering the concentration of gelrite, xanthan gum and HPMC as independent variables, gelation time, gel strength, and mucoadhesive force (N). Gelation time , gel strength, mucoadhesive force (N), viscosity (cP) and in vitro percentage drug release were chosen as dependent variables. The formulation was characteristics for pH, clarity, isotonicity, sterility, rheological behavior, and in vitro drug release, ocular irritation, and ocular visualization.Result: Based on desirability index of responses, the formulation containing a concentration of gelrite (0.4%), xanthan gum (0.21%), and HPMC (HPMC E50 (0.24%) was found to be the optimized formulation concentration developed by 23 factorial design. The solution eye drops resulted in an in situ phase change to gel-state when mixed with simulated tear fluid. The gel formation was also confirmed by viscoelastic measurements. Drug release from the gel followed non-fickian mechanism with 88% of drug released in 10 h, thus increased the residence time of the drug.Conclusion: An in situ gelling system is a valuable alternative to the conventional system with added benefits of sustained drug release which may ultimately result in improved patient compliance.

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Xyloglucan Based In Situ Gel of Lidocaine HCl for the Treatment of Periodontosis

Journal of Pharmaceutics ◽

10.1155/2016/3054321 ◽

2016 ◽

Vol 2016 ◽

pp. 1-9 ◽

Cited By ~ 6

Author(s):

Ashlesha P. Pandit ◽

Vaibhav V. Pol ◽

Vinit S. Kulkarni

Keyword(s):

Sol Gel ◽

Periodontal Pocket ◽

Lidocaine Hydrochloride ◽

Temperature Sensitive ◽

In Situ Gel ◽

Dental Surgery ◽

Fast Onset ◽

Tamarind Seed

The present study was aimed at formulating thermoreversible in situ gel of local anesthetic by using xyloglucan based mucoadhesive tamarind seed polysaccharide (TSP) into periodontal pocket. Temperature-sensitive in situ gel of lidocaine hydrochloride (LH) (2% w/v) was formulated by cold method. A full 32 factorial design was employed to study the effect of independent variables concentrations of Lutrol F127 and TSP to optimize in situ gel. The dependent variables evaluated were gelation temperature (Y1) and drug release (Y2). The results revealed the surface pH of 6.8, similar to the pH of saliva. Viscosity study showed the marked increase in the viscosity of gel at 37°C due to sol-gel conversion. TSP was found to act as good mucoadhesive component to retain gel at the site of application in dental pocket. Gelation of formulation occurred near to body temperature. In vitro study depicted the fast onset of drug action but lasting the release (90%) till 2 h. Formulation F7 was considered as optimized batch, containing 18% Lutrol F127 and 1% tamarind seed polysaccharide. Thus, lidocaine hydrochloride thermoreversible in situ gel offered an alternative to painful injection therapy of anesthesia during dental surgery, with fast onset of anesthetic action lasting throughout the dental procedure.

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THERMOREVERSIBLE IN-SITU NASAL GEL FORMULATIONS AND THEIR PHARMACEUTICAL EVALUATION FOR THE TREATMENT OF ALLERGIC RHINITIS CONTAINING EXTRACTS OF MORINGA OLIFERA AND EMBELIA RIBES

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2017v9i6.18780 ◽

2017 ◽

Vol 9 (6) ◽

pp. 16 ◽

Cited By ~ 1

Author(s):

Richa Srivastava ◽

Sajal Srivastava ◽

Satya Prakash Singh

Keyword(s):

Drug Delivery ◽

Allergic Rhinitis ◽

Nasal Cavity ◽

Xanthan Gum ◽

Drug Formulation ◽

Pluronic F127 ◽

Therapeutic Effects ◽

In Situ Gel ◽

Embelia Ribes

Objective: The present study was planned to develop thermo-reversible in-situ gel for the treatment of allergic rhinitis (AR). The objective of the present investigation was to develop a mucoadhesive in-situ gel with reduced nasal mucocilliary clearance to improve the local effect of the polyherbal extract in the treatment of allergic rhinitis (AR). The prolonged residence of drug formulation in the nasal cavity is one of utmost importance for intranasal drug delivery. The prepared formulations were subjected for gelling temperature, gelling time, viscosity, gel strength, pH, drug content, mucoadhesive strength, spread ability and irritancy studies.Methods: In the study the pluronic F127 (PF127) based mucoadhesive in-situ nasal gels containing Moringa olifera (MO) and Embelia ribes (ER) extracts were used having antioxidant and anti-inflammatory effect. A polyherbal thermosensitive in-situ hydrogel was designed and evaluated by the mixing of pluronic F127, poly (ethylene glycol) (PEG400) and Xanthan gum with a small amount of (hydroxypropyl methylcellulose) HPMC K4M and Carbopol 934. Total 13 thermosensitive in-situ gels of extracts were prepared through combination of HPMC K4M or Carbopol or xanthan gum and PF127. All the preparations were investigated, and the selected method for gel formation underwent the thermal transition from sol to hydrogel.Results: The mucoadhesive gel after being administered into the nasal cavity, get transformed into the viscous hydrogel at body temperature, which diminished nasal mucociliary clearance and prolonged the duration of action. The in-situ nasal herbal gel prepared by combination of different concentration of to HPMC K4M or carbopol or xanthan gum with PF127 (10% w/v) produces the better and effective gel. The findings of evaluation parameter indicate that the in-situ gel prepared by combination with corbopol were better quality compared to HPMC K4M and xanthan gum.Conclusion: From these findings, it can be concluded that in-situ herbal nasal gels may be potential drug delivery systems for Moringa olifera and Embelia ribes extracts to overcome first-pass metabolism and thereby to improve the bioavailability. The mucoadhesive in-situ gel system is a promising approach for the intranasal delivery of polyherbal extracts for the therapeutic effects improvement of Allergic rhinitis.

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A Novel Approach of Drug Localization through Development of Polymeric Micellar System Containing Azelastine HCl for Ocular Delivery

Pharmaceutical Nanotechnology ◽

10.2174/2211738507666190726162000 ◽

2019 ◽

Vol 7 (4) ◽

pp. 314-327

Author(s):

Sheetal Devi ◽

Vipin Saini ◽

Manish Kumar ◽

Shailendra Bhatt ◽

Sumeet Gupta ◽

...

Keyword(s):

Allergic Conjunctivitis ◽

Polymeric Micelles ◽

Ex Vivo ◽

Entrapment Efficiency ◽

Ph Sensitive ◽

Micellar System ◽

Ocular Delivery ◽

In Situ Gel ◽

Micelle Size

Background: Development of polymeric micelles for the management of allergic conjunctivitis to overcome the limitations of topical installation, such as poor patient compliance, poor stromal permeability, and significant adverse effects, increase precorneal residence time and efficacy, and also control the release of drug at the target site. Objective: The investigation was aimed at developing a polymeric micellar system of Azelastine HCl for Ocular Delivery. Methods: Drug loaded micelles of tri-block copolymers Pf 127 were prepared by Thin Film hydration method. The polymeric micelles formulations (F1 to F9) were assessed for entrapment efficiency, micelle size, in vitro permeation, ex vivo transcorneal permeation, in vivo Ocular Irritation, and Histology. Results: Optimized micelles formulation (F3), with the lowest micelle size of 92 nm, least polydispersity value of 0.135, highest entrapment efficiency of 95.30 ± 0.17%, and a cumulative drug permeation of 84.12 ± 1.26% in 8h, was selected to develop pH-sensitive micelles loaded carbopol in situ gel. The optimized in situ gel (G4) proved to be superior in its ex vivo transcorneal permeation when compared with Market Preparation and pure drug suspension, exhibiting 43.35 ± 1.48% Permeation with zero-order kinetics (r2 = 0.9944) across goat cornea. Transmission Electron microscopy revealed spherical polymeric micelles trapped in the gel matrix. A series of experiments showed hydration capability, non-irritancy, and histologically safe gel formulation that had appropriate handling characteristics. Conclusion: A controlled release pH-sensitive ocular formulation capable of carrying the drug to the anterior section of the eye via topical delivery was successfully developed for the treatment of allergic conjunctivitis.

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Design and optimization of novel in situ gel of mercaptopurine for sustained drug delivery

Brazilian Journal of Pharmaceutical Sciences ◽

10.1590/s1984-82502011000100011 ◽

2014 ◽

Vol 50 (1) ◽

pp. 107-119 ◽

Cited By ~ 7

Author(s):

R. Nagendra ◽

Roopa S. Pai ◽

Gurinder Singh

Keyword(s):

Sodium Chloride ◽

Xanthan Gum ◽

Oral Absorption ◽

In Vitro Dissolution ◽

Disintegration Time ◽

In Situ Gel ◽

Weight Variation ◽

Swelling Studies

Mercaptopurine is a purine antagonist, belonging to the class of antimetabolites. Its oral absorption is erratic and variable throughout GIT, with bioavailability of 5-37% and belongs to Biopharmaceutical Classification System (BCS) class IV. The focus of the present study was to improve solubility of mercaptopurine and to release the drug uniformly throughout the GIT by formulating into a novel in situ gel tablet. By in vitro swelling studies, xanthan gum was selected as the best gelling polymer and the tablets were prepared by direct compression. Sodium chloride was used as a release modifier to improve the release of drug from the tablet. A 32 full factorial design was applied to optimize the percentage of xanthan gum and sodium chloride to get desired swelling index and release profile. Tablets were evaluated for weight variation, hardness, friability, disintegration time, drug content, in vitro swelling studies and in vitro dissolution studies. The best optimized formulation showed good swelling index and extended the release up to 12 h, where as conventional tablet released the drug within 45 min. The results indicate that mercaptopurine loaded in situ gel tablet could be effective in sustaining drug release for a prolonged period of time throughout the GIT, which can possibly improve the oral bioavailability.

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FORMULATION AND EVALUATION NASAL IN SITU GEL OF RIZATRIPTAN

International Journal of Pharmacy Research & Technology ◽

10.31838/ijprt/09.02.03 ◽

2019 ◽

Vol 9 (2) ◽

Keyword(s):

In Situ Gel

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Scaffolds for Drug Delivery in Tissue Engineering

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2008.1.2.1 ◽

2008 ◽

Vol 1 (2) ◽

pp. 113-123 ◽

Cited By ~ 2

Author(s):

Vikas V. Gaikwad ◽

Abasaheb B. Patil ◽

Madhuri V. Gaikwad

Keyword(s):

Drug Delivery ◽

Tissue Engineering ◽

Heart Diseases ◽

Cartilage Regeneration ◽

Tissue Growth ◽

The Body ◽

Patient Specific ◽

In Situ Gel ◽

Heart Muscle Cells

Scaffolds are used for drug delivery in tissue engineering as this system is a highly porous structure to allow tissue growth. Although several tissues in the body can regenerate, other tissue such as heart muscles and nerves lack regeneration in adults. However, these can be regenerated by supplying the cells generated using tissue engineering from outside. For instance, in many heart diseases, there is need for heart valve transplantation and unfortunately, within 10 years of initial valve replacement, 50–60% of patients will experience prosthesis associated problems requiring reoperation. This could be avoided by transplantation of heart muscle cells that can regenerate. Delivery of these cells to the respective tissues is not an easy task and this could be done with the help of scaffolds. In situ gel forming scaffolds can also be used for the bone and cartilage regeneration. They can be injected anywhere and can take the shape of a tissue defect, avoiding the need for patient specific scaffold prefabrication and they also have other advantages. Scaffolds are prepared by biodegradable material that result in minimal immune and inflammatory response. Some of the very important issues regarding scaffolds as drug delivery systems is reviewed in this article.

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