Formulation development of smart gel periodontal drug delivery system for local delivery of chemotherapeutic agents with application of experimental design

Dabhi, Mahesh R.; Nagori, Stavan A.; Gohel, Mukesh C.; Parikh, Rajesh K.; Sheth, Navin

doi:10.3109/10717544.2010.490247

Cited by 41 publications

(22 citation statements)

References 30 publications

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“…Drug concentration in filtrated solution was determined spectrophotometrically at 257 nm using UV-Visible spectrophotometer (Shimadzu 1700, Japan). [20]…”

Section: Methodsmentioning

confidence: 99%

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Formulation and evaluation of periodontal in situ gel

Garala

Joshi

Shah

et al. 2013

Int J Pharma Investig

142

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Background:The present study was aimed to develop and optimize in situ gel for the treatment of periodontal disease.Materials and Methods:Temperature-sensitive in situ gel containing 0.1% w/v Chlorhexidine hydrochloride was formulated by cold method using different polymers. Preliminary study was carried out to optimize different types and concentration of polymers such as Poloxamer 188, Poloxamer 407, Gellan gum, and Carbopol 934P. Central composite design was employed for optimization of the effect of independent variables such as Poloxamer 407 and Carbopol 934P on responses such as gelation temperature, spreadability, cumulative percentage release at 2 h, and time for 50% drug release (t50 %). Each formulations were evaluated for clarity, pH, gelation temperature, spreadability, drug content, in vitro drug release, t50 %, and cumulative percentage drug release at 2 h.Results:Results of evaluation parameters revealed that the drug release, gelation temperature was considerably decreased with increasing t50 % as the concentration of each polymer was increased. The desirability function was utilized to find out optimized formulation of the factorial design. Formulation F6 showed the highest overall desirability of 0.6283 and, therefore, this formulation was considered to be the optimized formulation. The % relative error was calculated, which showed that observed responses were in close agreement with the predicted values calculated from the generated regression equations.Conclusion:The clarity, pH, drug content of all formulations was found to be satisfactory. Further, all the formulations showed sustained drug release for a period of 6 h, which satisfied to treat periodontal disease.

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“…Drug concentration in filtrated solution was determined spectrophotometrically at 257 nm using UV-Visible spectrophotometer (Shimadzu 1700, Japan). [20]…”

Section: Methodsmentioning

confidence: 99%

“…62 at the speed of 50 rpm in the sample, and the viscosity was measured at 10 min after the rotation of the spindle. [2026]…”

Section: Methodsmentioning

confidence: 99%

Formulation and evaluation of periodontal in situ gel

Garala

Joshi

Shah

et al. 2013

Int J Pharma Investig

142

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“…The measurements were done 10 min after the dipping of spindle no. 62, which was rotating at a speed of 50 rpm [31,32]. Viscosity was measured before and after the gelation of the formulation.…”

Section: Determination Of Viscositymentioning

confidence: 99%

Preparation and Optimization of In Situ Gel Loaded with Rosuvastatin-Ellagic Acid Nanotransfersomes to Enhance the Anti-Proliferative Activity

2020

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The objective of this study was to develop an optimized sustained-release nanotransfersomes (NTS) based in situ gel formulation of rosuvastatin (RO) combined with ellagic acid (EA) antioxidant, to enhance cytotoxic and anti-proliferative activity against tongue carcinoma. The concentrations of lecithin, Tween 80, and d-tocopherol polyethylene glycol succinate (TPGS) were considered as independent variables. Particle size, entrapment, and stability were selected as dependent variables. The obtained formulation containing 25% lecithin, 20% Tween 80, and TPGS 15% fulfilled the prerequisites of the optimum formulation. RO-NTS loaded in situ gel was prepared and optimized for concentrations of Poloxamer 407, and Carbopol, using statistical design. Drug release from in situ gel showed a sustained release profile. The RO IC50 was decreased by half for the in situ gel in comparison to plain RO and RO-EA-NTS. A significant amount of caspase-3 was detected in all the formulation treatments. The studies indicated that EA's synergistic anti-oxidant effect owing to a high affinity to the PGP efflux transporter and higher penetration in the RO-NTS formulation led to a higher inhibition against human chondrosarcome-3 cancer cell lines. RO-EA NTS-loaded in situ gel had a sustained release that could be significant in localized therapy as an alternative to surgery in the treatment of aggressive tongue carcinoma. sensitivity of lung cancer and human leukemia cell lines to anthracyclines [6,7]. Administration of statins combined with antioxidant compounds of natural origin can yield better results as shown in the combination of simvastatin and alpha-lipoic acid that improved toxicity against breast carcinoma cell lines [8].Transferosomes, defined as vesicular colloidal dispersions composed mainly of phospholipids and nonionic surfactants acting as edge activators (EA), have attracted a great deal of attention in the field of drug delivery [9]. The presence of such EA weakens the bonds between phospholipids molecules and imparts the property of elasticity onto transferases making them ultra deformable vesicles. Transferosomes have several advantages that make them successful vesicular drug delivery systems, including (a) being biodegradable and biocompatible with human body, and (b) the ability of EA to solubilize and stabilize poorly soluble drugs owing to their surface activity, low toxicity, enhanced tissue targeting capacity, and ability to obtain prolonged drug release [10][11][12]. RO, also known as "superstatin," is the most effective antihyperlipidemic agent in the statins family. It is more efficient and attains fewer side effects compared to other statins although it exhibits poor solubility and poor bioavailability [13]. Several studies have proven the anticancer activity of RO. It showed cytotoxic effects against thyroid cancer cells in vitro as it increased the caspase-3 activity and apoptosis confirmed by DNA fragmentation analysis [14], and reduced viability in cervical, hepatic, and breast cancer cell lines [15]. Mor...

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“…The developed in situ gel formulations were evaluated for pH using calibrated digital pH meter that calibrated before each use with standard pH 4, 7, and 9.2 buffer solutions. The formulation maintained at 25°C and all measurements were performed in triplicate (Dabhi et al, 2010;Niranjan et al, 2013).…”

Section: In Vitro Characterizationmentioning

confidence: 99%

In vitro and in vivo evaluation of an in situ forming gel system for sustained delivery of Florfenicol

Liu

et al. 2014

Vet Pharm & Therapeutics

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The objective of this study was to develop an injectable in situ forming gel system based on Poloxamer for sustained release of Florfenicol (FFC). The formulations were prepared containing certain amounts of Poloxamer 407 (P407) and Poloxamer 188 (P188) alone or with hydroxylpropyl methylcellulose (HPMC), sodium carboxymethyl cellulose (CMC-Na), or polyvinyl pyrrolidone (PVP) as polymer additives. The optimal formulation was chosen according to in vitro parameters (gelation temperature, gelation time, pH value, viscosity, and in vitro release). Then the FFC in vivo pharmacokinetic character of the optimal formulation was investigated in dogs with a single dose of 50 mg/kg b.w. under s.c. injection. In vitro release studies, all formulations containing polymer additives had prolonged release time and decreased initial burst to some extent. The optimal formulation containing 0.15% HPMC showed a best sustained release profile for about 128 h with the lowest initial burst in vitro (<40% in 24 h). In vivo, the 20% FFC in situ forming gel provided prolonged drug release time within the therapeutic range for about 100 h, with stable plasma levels and elimination half-life (t1/2λz ) nine times higher than the control formulation. In conclusion, in situ forming gel is an attractive alternative for FFC sustained release system.

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Formulation development of smart gel periodontal drug delivery system for local delivery of chemotherapeutic agents with application of experimental design

Abstract: (2010) Formulation development of smart gel periodontal drug delivery system for local delivery of chemotherapeutic agents with application of experimental design, Drug Delivery, 17:7, 520-531,

Cited by 41 publications

References 30 publications

Formulation and evaluation of periodontal in situ gel

Formulation and evaluation of periodontal in situ gel

Preparation and Optimization of In Situ Gel Loaded with Rosuvastatin-Ellagic Acid Nanotransfersomes to Enhance the Anti-Proliferative Activity

In vitro and in vivo evaluation of an in situ forming gel system for sustained delivery of Florfenicol

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