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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In this research, we prepared a polymer blend of polyvinylalcohol (PVA)/carrageenan/kaolinite by means of the solution cast approach. The composition of the blend was PVA in 1 gm by weight with 0.2 gm carrageenan as a plasticizer. The ratio of nanoclay varied between 1 and 5 wt%. Different properties were investigated in this study such as water vapor permeability, hardness, tear strength, color stability, thermal stability, and antibacterial activity. Water vapor permeability was decreased with increasing the ratio of nanoclay, while the values of hardness, tear strength, color stability, and thermal stability were increased. Also, the antibacterial activity examination with two types of bacteria, e.g.
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Lasmiditan (LAS) was formulated as a nanoemulsion based in situ gel (NEIG)with the aim of improving its oral bioavailability via application intranasally. The solubility of LAS in oils, emulsifiers, and co-emulsifiers was determined to identify nanoemulsion (NE)components. Phase diagrams were constructed to identify the area of nanoemulsification. LAS NE was formulated using the spontaneous nanoemulsification method. Four NEs (F19, F24, F31, and F34) containing 7-15 % oleic acid (OA) as an oily phase, 40-55% labrasol (LR), and transcutol (TC) as emulsifier mixture at (1:1), (2:1), (3:1), and (1:2) ratio with 30-53 % (w/w) aqueous phase, having suitable optical transparency of 95–98%, globule size of 104-140 nm and polydisper
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By using precipitation polymerization, liquid electrodes of polymers imprinted with Mebeverine hydrochloride and metronidazole benzoate were created whereas the imprinted polymer (MIP) and non imprinted (NIP) polymers were prepared by using Mebeverine hydrochloride and Metronidazole benzoate qua a template. In the polymerization process, 2-Acrylamido-2-methyl-1-propane Sulphonic acid (AMPS) or 1-Vinylimidazole (VIZ) was used qua monomer, pentaerythritol triacrylate (PETRA) or Divinylbanzene (DVB) was used qua a cross-linker while benzoyl peroxide (BPO) was used as an initiator. The MIP membranes and the membranes of NIP were created by using Dibutyl Sebacate (DBS) and Tris(2-ethylhexyl)phosphate(TEHP) qua plasticizers
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Background Idebenone is an extensively metabolized drug with poor water solubility that is used to treat Leiber’s hereditary optical neuropathy.
Objective This study aims to prepare idebenone nanoemulsion as a poloxamer-based nasal gel to overcome the extensive rate of hepatic metabolism for better bioavailability and lower histopathological effect on the nasal mucosa.
Methods The formulation strategy was based on eliciting mutual concentration reduction between the nanoemulsion and the carrier gel by setting their gelation temperature between 30-32°C to overcome the mucociliary dose washout. The o/w nanoemulsions rely on cremophor EL and transcutol as an emulsifying sys
... Show MoreThis research aims to develop transdermal patches of Ondansetron hydrochloride (OSH) with different types of polymers, ethyl cellulose and, polyvinyl pyrrolidone k30 in a ratio (3:0.5,3:1,3:2,2:1,1:1) with propylene glycol 20%w/w as a plasticizer. Prepared transdermal patches were evaluated for physical properties. The compatibility between the drug and excipients was studied by Differential scanning calorimetry (DSC), where there is no interaction between the drug and polymers. From the statistical study, there is a statistical difference between all the prepared formulations p<0.05. In-vitro Release study of transdermal patches was performed by using a paddle over the disc. The release profile of OSH follow
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