scholarly journals Development and Statistical Optimisation of Buspirone Hydrochloride Buccoadhesive Films

2014 ◽  
Vol 2014 ◽  
pp. 1-12
Author(s):  
Upendra Nagaich ◽  
Vandana Chaudhary ◽  
Jaya Nagaich

The aim of the present study was to prepare unidirectional buccal films of buspirone hydrochloride by solvent casting technique. Hydroxypropylmethylcellulose (HPMC K15M) and Eudragit RL-100 were used as polymers in different proportion. Polyethylene glycol 400 and sodium lauryl sulphate were used as plasticizer and permeation enhancer, respectively, in different concentration. In the formulation, total amount of polymer (X1) and percentage of HPMC K15M (X2) were kept as independent variables. Afterwards, statistically optimized process was carried out and two optimized formulations (OF1 and OF2) were developed. The observed results of optimized formulation were showed a greater degree of percentage of similarity with predicted values. The stability studies showed that there was no significant change found in physicochemical properties, in-vitro release, and ex-vivo diffusion studies.

Author(s):  
Mona Semalty ◽  
Ajay Semalty ◽  
Ganesh Kumar ◽  
Vijay Juyal

For improving bioavailability in controlled release fashion and to circumvent the hepatic first pass effect of glipizide mucoadhesive buccal films of glipizide were prepared by solvent casting technique. Buccal films were prepared using hydroxy propylmethylcellulose, sodium carboxymethylcellulose, carbopol-934P and Eudragit RL-100. Films were evaluated for their weight, thickness, surface pH, swelling index,       in vitro residence time, folding endurance, in vitro release, ex vivo permeation studies and drug content uniformity. The films exhibited controlled release over more than 6 h. From the study it was concluded that the films containing 5 mg glipizide in 4.9 % w/v hydroxy propylmethylcellulose and 1.5 % w/v sodium carboxymethylcellulose exhibited satisfactory swelling, an optimum residence time and promising drug release thus proved to be potential candidate for the development of buccal films for therapeutic use.


Author(s):  
Sudhakar Beeravelli ◽  
Vyasamurthy Akondi ◽  
Madhavi Nimmathota

Aim: Aim of the present study is to develop and characterize simvastatin niosomal film for effective buccal delivery. Methods: Simvastatin niosomes were developed by film hydration technique followed by high-pressure homogenization using chiller at 5°C. The simvastatin niosomes were characterized for various physicochemical parameters and simvastatin plain and niosomal films were prepared using PEO as the base by solvent casting technique. Results: From the simvastatin niosomes suspension, the percentage assay was found in the range of 96 to 103%, particles size was found in the range of 112nm to 308nm, the zeta potential was found in the range of -9 to -25.8mV, the %EE was found in the range of 28% to 91% and the in vitro permeation was found in the range of 43.41% to 98% respectively. The niosomal film shown superior results as compared to simvastatin plain film. The FTIR and DSC confirm the compatibility among the existed excipients. Conclusion: Niosomes alter the physicochemical properties of simvastatin by buccal route. The prolonged permeation (96.12% up to 24hrs) of simvastatin was observed from niosomes film across the porcine buccal cavity, due to the presence of CPE in the composition, which would be useful for effective buccal delivery.


Author(s):  
Prasanta Kumar Mohapatra ◽  
Boddu Pavan Kumar ◽  
Pankaj Singh Patel ◽  
Harish Chandra Verma ◽  
Satyajit Sahoo

Mucoadhesive buccal films of rivastigmine were prepared by the solvent casting technique using HPMC K15M, sodium alginate, glycerine, and Eudragit RL100. Arranged films assessed for weight variation, thickness, % drug substance, % moisture loss, % moisture take-up, folding endurance, in-vitro medicament release, and Fourier transform Infrared spectroscopy (FTIR). The films showed a controlled release (CR) over 8 h. The preparation observed to be a worthy candidate for the development of buccal patches for therapeutic purposes. Drug-polymer compatibility considers FTIR demonstrated no contradiction between the medicament and the polymers. The optimized formulation found F7 indicated drug release 85% at the end of 8 h. Thinking about the correlation coefficient (R2) values got from the kinetic equations, the drug release from the formulations F1-F8 has discovered zero-order release mechanism. It can be concluded that oral buccal patches of rivastigmine, for treatment of Alzheimer’s and Parkinson’s disease, can be formulated. The study suggests that rivastigmine can be conveniently administered orally in the form of buccal patches, with the lesser occurrence of its side effects and improved bioavailability.


Author(s):  
Mohammad Muqtader Ahmed ◽  
Farhat Fatima ◽  
Abdul Bari Mohammed

The objective of the study was to formulate olive oil based organogels for the topical application of fluconazole (FLZ), to ensure the efficient delivery of the drug deeper in to the skin layers. Methods: Nine formulations developed by hot-melt method using olive oil, sorbitan monostearate (SMS) and FLZ. Prepared formulations characterized for macro evaluations, pH, spreadibility, viscosity, gel-sol transition, in-vitro diffusion study. Further optimized formulation evaluated for ex-vivo percutaneous permeation, in-vitro antifungal studies and stability studies by similarity index. Results: The results of evaluated parameters ensure the stability and effectiveness of the prepared olive oil based organogels. In-vitro diffusion studied reflects decrease in drug release with increase in surfactant concentration due to increase in viscosity. Moreover, ex-vivo permeation studies revealed that the permeation of FLZ was enhanced for optimized formulations (F6) as compared to the marketed gel formulation. Further, the optimized formulation exhibits the broad zone of inhibition against fungal strains in comparison to control and marketed product during in-vitro antifungal study. Conclusion: The olive oil based organogels formulation shown the enhanced permeation of FLZ from organogel network structure with good antifungal activity as compared to the marketed formulation. Henceforth, the FLZ organogel formulations could be used topically for the effective treatment of fungal infection.


Author(s):  
Sheikh Sofiur Rahman ◽  
ABDUL BAQUEE AHMED

Objectives: The main objective of this study was to develop and evaluate Nevirapine nanoparticle loaded mucoadhesive gel (NVP-Np mucoadhesive gel) for vaginal application for the treatment of HIV infection.  Methods: NVP loaded nanoparticles were prepared by salting out method followed by incorporation in different gel bases to produce NVP-Np mucoadhesive gel The prepared gels were evaluated for their physicochemical parameters, rheological characteristics, mucoadhesion, in-vitro drug release and ex-vivo permeation of drug across porcine vaginal mucosa.  Results: The result of FT-IR and DSC study confirmed the absence of incompatibility of NVP with excipients used in the formulations. The particle size of the prepared NVP-Np was found to be 243.8 ± 3.15 nm, a polydispersity index (PI) of 0.787± 0.002 and zeta potential value -17.12 mV, which revealed the stability of nanoparticles. All the formulations showed good homogeneity, spreadability, physical appearance and content uniformity. The pH of the mucoadhesive gel formulations was in the range of 3.70 ± 0.03 to 4.56 ± 0.02, which lies in the normal pH range of the vaginal fluid.  The cumulative amounts permeated at 6 h were 832.23 ± 63.45 μg/cm2 , 592.13 ± 82.55 μg/cm2 and 941.32 ± 81.10 μg/cm2 from F1(1% Chitosan), F2(1% Carbopol 974P) and F3 (1% HPMC K100M )  respectively. A linear relationship [r2 > 0.9 (0.97 n 0.99)] was observed between the percentage cumulative amount permeated and time, indicating zero order kinetics. Conclusion: In conclusion, NVP-Np mucoadhesive gel was prepared successfully using salting out followed by a homogenization technique for vaginal application of NVP for the prophylaxis of HIV infection.


2021 ◽  
Vol 20 (11) ◽  
pp. 2241-2248
Author(s):  
M. Yasmin Begum ◽  
Ali Alqahtani

Purpose: To formulate and characterize tizanidine hydrochloride (TZN) and piroxicam (PRX)-loaded bilayer mucoadhesive buccal films with an intention to improve the bioavailability and patient compliance in pain management.Methods: Bilayer buccal films were prepared by solvent evaporation technique using hydroxypropyl methylcellulose (HPMC) 15cps and polyvinylpyrrolidone (PVP K30 as immediate release (IR) layer forming polymers and HPMC K15 M, PVP K 90 along with various muco adhesive polymers (Carbopol P934, sodium alginate, etc), as sustained release (SR) layer forming polymers. The prepared films werecharacterized for thickness, weight variation, folding endurance, surface pH, swelling index,mucoadhesive strength, in vitro residence time, in vitro drug release, ex vivo permeation and drug release kinetics.Results: The prepared films were of largely uniform thickness, weight and drug content. Moisture loss (%) and folding endurance were satisfactory. Surface pH was compatible with salivary fluid. Disintegration time was 85 s for F1 and 115 s for F2 of IR films. In vitro dissolution studies showed 99.12 ± 1.2 % (F1) and 90.36 ± 1.8 % (F2) were released in 45 min. Based on the above results, F1 was chosen as the optimum formulation to be combined with SR layer of TZN. Amongst the SR layers of TZN in vitro drug release. The findings show that of F2 was 98.38 ± 0.82 % and correlated with ex vivo release. Drug release followed zero order release kinetics and mechanism of drug release was non-Fickian type diffusion. In vitro residence time was greater than 5 h.Conclusion: The findings show that the bilayer buccal films demonstrate the dual impact of deliveringPRX instantly from the IR layer, with good controlled release and permeation of TZN from the SR layer, thus providing enhanced therapeutic efficacy, drug bioavailability and patient compliance.


2021 ◽  
Vol 62 (3) ◽  
pp. 290-304
Author(s):  
Moreshwar Patil ◽  
Prashant Pandit ◽  
Pavan Udavant ◽  
Sandeep Sonawane ◽  
Deepak Bhambere

Introduction: Etodolac is used in the treatment of acute pain and inflammation. It has low solubility because of high hydrophobicity and it is reported that upon oral administration shows gastric disturbances. This encourages the development of topical vesicular formulation. Method: In this work we used coacervation-phase separation method for the development of etodolac loaded vesicular system by using non-ionic surfactants, cholesterol and soya lecithin. Central composite design (rotatble) was used to optimize the concentrations of soy lecithin, surfactant and cholesterol. The prepared formulations were characterized by number of vesicles formed, vesicle size, zeta potential, entrapment efficiency, in-vitro permeation, ex-vivo permeation and anti-inflammatory study. Results: Etodolac was successfully entrapped in all formulations having efficiency in the range of 74.36% to 90.85%, which was more at 4 °C than room temperature. When hydrated with water; niosome in the range of 54 to 141 (per cubic mm) were spontaneously produced. The results of in-vitro diffusion study revealed that etodolac was released in the range of 71.86 to 97.16% over a period of 24 hrs. The average vesicle size of optimized formulation was found 211.9 nm with PDI of 0.5. The observed responses i.e. % encapsulation efficiency and drug release were 74.12 and 95.08 respectively. The zeta potential was -19.4mV revealed the stability of formulation which was further confirmed by no changes in drug content and drug release after stability studies. The % inhibition in paw volume was 40.52% and 43.61% for test and marketed proniosomal gel. Conclusion: Proniosomal gel formulation was stable and could enhance skin delivery of etodolac because of excellent permeation capability of vesicular system.


2019 ◽  
Vol 144 ◽  
pp. 180-192 ◽  
Author(s):  
Georgios K. Eleftheriadis ◽  
Christos Ritzoulis ◽  
Nikolaos Bouropoulos ◽  
Dimitrios Tzetzis ◽  
Dimitrios A. Andreadis ◽  
...  
Keyword(s):  
Ex Vivo ◽  

Author(s):  
Shayeda ◽  
Sathish Dharani

The goal of the present investigation was to design and evaluate mucoadhesive buccal patches of Ondansetron Hydrochloride (OND) which is used for nausea and vomiting associated with cancer chemotherapy and radiotherapy. Permeation of OND was calculated ex vivo using porcine buccal membrane. Buccal films were developed by solvent-casting technique using Hydroxy Propyl Methyl Cellulose(HPMC E15) as mucoadhesive polymer. The patches were evaluated for weight variation, thickness variation, surface pH, moisture absorption, in vitro residence time, mechanical properties, in vitro release, ex vivo permeation studies and drug content uniformity. The formulation F3 was found to give the better results and obeys first order kinetics. 


INDIAN DRUGS ◽  
2016 ◽  
Vol 53 (09) ◽  
pp. 34-41
Author(s):  
M. R Andrea ◽  
◽  
P. M. Dandagi ◽  
A. P. Gadad

The aim of the present study was to develop a fast dissolving buccal film of dimenhydrinate with good mechanical properties and fast disintegration, producing an acceptable taste when placed in the mouth. The formulations were developed by solvent casting method by using HPMC E5 and HPMC E15 as film formers in different concentrations, propylene glycol as plasticizer and Poloxamer 407 as solubiliser. The resultant films were evaluated for various parameters. the films were found to be satisfactory for all the parameters. All formulations released more than 85% of the drug within 15 minutes. Formulation F7 (1% HPMC E5: 1% HPMC E15) was selected as the optimized formulation based upon the least disintegration time (24.3sec), optimum mechanical properties, percentage drug content (94.96%) and in vitro drug release (95.20%). The ex vivo release was found to be acceptable. Stability studies revealed that the formulation was stable on storage for two months.


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