scholarly journals Design, Optimization and Evaluation of Snedds Based System for Orlistat: A Quality by Design Approach With 23 Factorial

2020 ◽  
Vol 11 (4) ◽  
pp. 5517-5532
Author(s):  
Amisha Vyas ◽  
Anupama Diwan ◽  
Rupali Sharma

Obesity, as defined by WHO is an abnormal or excessive fat accumulation that may impair health. is directly proportional to the resultant impact of genetic, metabolic, environment, and culture issues. The leading cause of obesity is an energy imbalance between calories consumed and calories exhausted. To design and optimize SNEDDS formulation by the development of SNEDDS with an appropriate quantity of oil, and with the factorial approach. A series of SNEDDS formulations for was prepared based on solubility studies, pseudo ternary phase diagram and visual observation. was added inaccurately weighed amount of oil into a screw-capped glass vial and heated in a water bath at 40ºC. The and were added to the oily mixture and stirred with a magnetic bar. The formulation was further for 15 minutes and stored at room temperature. From the result of evaluation parameters such as emulsification time 6±1s, % transmittance 94.01±1.5%, drug Loading 99.89%±0.56%, Index 0.47±0.01 and 0.211±0.02, Globulesize99±6 nm, Zeta potential -28.12 and -24.5 , The , Freeze-thaw cycle, Heating-cooling cycle showed no signs of phase separation, Viscosity 132.4±0m Pa.s, drug release 99.25% within 90 minutes, drug release follows Korsmeyer-Peppas model mechanism, n value was found to be1.083 hence it can be postulated formulation F-6 followed the or anomalous release and P-value for factors emulsification time, % transmittance and % drug release was found less than 0.0500 and hence it was concluded formulation F-6 an optimized formulation.

2021 ◽  
Vol 10 (24) ◽  
pp. 5762
Author(s):  
Vidán-Estévez Vidán-Estévez ◽  
Sánchez-Herráez Sánchez-Herráez ◽  
Escalante-Barrigón Escalante-Barrigón ◽  
Seco-Calvo Seco-Calvo

Chronic non-healing wounds (CNHWs) may be associated with trauma or idiopathic in nature and are difficult to treat. Our objective was to assess the use of platelet-derived growth factor (PDGF) from single-donor platelets (al-PRP), using one freeze-thaw cycle, for treating CNHWs. We conducted a cross-sectional study. A total of 23 CNHWs being treated with al-PRP. The al-PRP treatment can be considered successful in well over half (n = 13, 56.5%) of the wounds. We found that all the wounds treated for up to 7 weeks showed partial or complete healing, while those treated for between 8 and 12 weeks did not show healing, healing again being successful in cases in which treatment was extended to more than 13 weeks (85.7%). Using chi-square tests, this relationship was found to be highly significant (p < 0.001, chi2 = 19.51; p value = 0.00006). Notably, Cramer’s V coefficient was very high (0.921), indicating that the effect size of PRP treatment duration on healing is very large (84.8%). We could suggest that the use of al-PRP in the healing of CNHWs is a promising approach. Further studies with larger sample sizes and long follow-ups are needed to obtain multivariate models to explain which factors favour the healing of ulcers treated with PRP


2020 ◽  
Vol 27 (1) ◽  
pp. 131-138
Author(s):  
Leonny Yulita Hartiadi ◽  
Agnes Anania Triavika sahamastuti ◽  
Cynthia Valentina Chandra ◽  
Erlina Febriani ◽  
Shakila Angyaja Adiyanto ◽  
...  

Background: The excessive generation of ROS in the skin results in oxidative stress that can contribute to premature skin aging, inflammation, and skin carcinogenesis. To prevent these detrimental effects, the development of herbal medicine with a potent antioxidant activity into cosmetic products is required. This study aims to formulate cream that contains a safe and effective concentration of merbau (Intsia bijuga), which has been shown to have a strong antioxidant activity. Methods: Powdered merbau wood was macerated with methanol and the dried extract was evaluated for its cytotoxic effect and antioxidant activity on human keratinocytes cell line using MTS assay. Five cream formulations containing the extract were made and subjected to stability and physical evaluations, including organoleptic, types of cream, pH, viscosity, and homogeneity. Results: Cytotoxicity assay revealed that merbau extracts had an IC50 of 181.3 μg/mL (95% confidence interval (CI): 165.4 - 200.1 µg/mL). At a concentration of 31.25 μg/mL, the extract exhibited a protective effect against H2O2-induced oxidative stress, comparable to vitamin E. Five cream formulas that were developed demonstrated good physical properties that fulfilled the evaluation parameters, including o/w type of cream, homogenous, and stable based on centrifugation and freeze-thaw cycle tests. The pH values were between 5.65 ± 0.067 - 7.4 ± 0.050, while the viscosity values were between 131 ± 1.249 - 56,011 ± 2,729.27 mPa.s. All cream formulas exhibited shear-thinning properties upon increasing shear stress. Conclusion: Overall, this study has successfully formulated several cream formulations containing merbau extract at a concentration that shows antioxidant activity.


2021 ◽  
pp. 095646242110414
Author(s):  
Mohammad Shahidi-Dadras ◽  
Nasim Gholizadeh ◽  
Sahar Dadkhahfar ◽  
Mehdi Gheisari ◽  
Parsa Heydarifakher ◽  
...  

Bleomycin is an antineoplastic agent, which is used off label for various dermatologic conditions. There are numerous reports on the use of intralesional bleomycin (ILB) for the treatment of common warts. However, reports on the efficacy of bleomycin in the treatment of anogenital warts (AGWs) are still limited. The aim is to compare the efficacy/tolerability and recurrence rates of AGW treatment with ILB versus cryotherapy. In this prospective study, 50 patients with AGWs were assigned either to receive triple freeze–thaw cycle of cryotherapy or to receive 1.5 mg/mL ILB for a maximum of four sessions with 3-week intervals. Clinical efficacy was determined by the percentage of the patients with complete clearance. The patients with complete clearance were visited by passing 3 months from the last treatment session to evaluate any recurrence. Of 44 patients completing the study, 16 of 21 (76.19%) patients in the ILB group and 15 of 23 (65.22%) patients in the cryotherapy group showed complete resolution ( p value = .425). Moreover, recurrence occurred after 3 months in 18.75% and 46.66% of the ILB and the cryotherapy groups’ patients, respectively ( p value = .096). The most common local adverse events in both treatment groups were pain, dyspigmentation, and ulceration/erosion, while the delayed ulceration and secondary infection were only observed in the bleomycin group. Intralesional bleomycin is as effective as cryotherapy in the treatment of AGWs, but it is more invasive and associated with post-treatment pain, the delayed ulceration, and cutaneous infection. Intralesional bleomycin is not accompanied with the major risk of necrosis or fibrosis, so the use of ILB in the anogenital area is likely to be safe. This clinical trial was registered in Iranian Registry of Clinical Trials site with code: IRCT20190519043631N1.


Author(s):  
Tulsi Bisht ◽  
Rishishwar Poonam

The aim of present work was to develop once daily sustained release matrix tablet of aceclofenac by wet granulation technique using natural gums i.e.: gum acacia, guar gum and Xanthan gum. In this present study matrix tablets were prepared using three different methods and a comparative study was done. Aceclofenac sodium being the newer derivative of diclofenac having short biological half life (4hrs.), so it requires more than one dose per day to maintain therapeutic dose. The prepared tablets were evaluated for various parameters like weight variation, hardness, swelling index, friability, percent drug release and various release profile like zero order, first order, Higuchi's, and Koshemeyrs-peppa. All the evaluation parameters met pharmacopoeial specifications and through dissolution studies it was matrix tablets prepared with method 2 shows heighest percent drug release and matrix tablet prepared by method 3 showed lowest percent drug release at the end of 8 hrs. (Shown in fig. 8, comparative release study of all three formulations). Matrix tablet of aceclofenac were successfully prepared and evaluated and it can be concluded that matrix tablet prepared with natural gums showed release rate for a prolonged time and can be of great importance for “once daily” tablet to reduce side effects and toxicity related with NSAIDs.  


Author(s):  
Rajkumar Aland ◽  
Ganesan M ◽  
P. Rajeswara Rao ◽  
Bhikshapathi D. V. R. N.

The main objective for this investigation is to develop and optimize the solid lipid nanoparticles formulation of acitretin for the effective drug delivery. Acitretin loaded SLNs were prepared by hot homogenization followed by the ultrasonication using Taguchi’s orthogonal array with eight parameters that could affect the particle size and entrapment efficiency. Based on the results from the analyses of the responses obtained from Taguchi design, three different independent variables including surfactant concentration (%), lipid to drug ratio (w/w) and sonication time (s) were selected for further investigation using central composite design. The  lipid Dynasan-116, surfactant poloxomer-188 and co surfactant egg lecithin resulted in better percent drug loading and evaluated for particle size, zeta potential, drug entrapment efficiency, in vitro drug release and stability. All parameters were found to be in an acceptable range. TEM analysis has demonstrated the presence of individual nanoparticles in spherical shape and the results were compatible with particle size measurements.  In vitro drug release of optimized SLN formulation (F2) was found to be 95.63 ± 1.52%, whereas pure drug release was 30.12 after 60 min and the major mechanism of drug release follows first order kinetics release data for optimized formulation (F2) with non-Fickian (anomalous) with a strong correlation coefficient (R2 = 0.94572) of Korsemeyer-Peppas model. The total drug content of acitretin gel formulation was found to 99.86 ± 0.012% and the diameter of gel formulation was 6.9 ± 0.021 cm and that of marketed gel was found to be 5.7 ± 0.06 cm, indicating better spreadability of SLN based gel formulation. The viscosity of gel formulation at 5 rpm was found to be 6.1 x 103 ± 0.4 x 103 cp. The release rate (flux) of acitretin across the membrane and excised skin differs significantly, which indicates about the barrier properties of skin. The flux value for SLN based gel formulation (182.754 ± 3.126 μg cm−2 h−1) was found to be higher than that for marketed gel (122.345 ± 4.786 μg cm−2 h−1). The higher flux and Kp values of SLN based gel suggest that it might be able to enter the skin easily as compared with marketed gel with an advantage of low interfacial tension of the emulsifier film that ensures an excellent contact to the skin. This topically oriented SLN based gel formulation could be useful in providing site-specific dermal treatment of psoriasis


2020 ◽  
Vol 27 (22) ◽  
pp. 3623-3656 ◽  
Author(s):  
Bruno Fonseca-Santos ◽  
Patrícia Bento Silva ◽  
Roberta Balansin Rigon ◽  
Mariana Rillo Sato ◽  
Marlus Chorilli

Colloidal carriers diverge depending on their composition, ability to incorporate drugs and applicability, but the common feature is the small average particle size. Among the carriers with the potential nanostructured drug delivery application there are SLN and NLC. These nanostructured systems consist of complex lipids and highly purified mixtures of glycerides having varying particle size. Also, these systems have shown physical stability, protection capacity of unstable drugs, release control ability, excellent tolerability, possibility of vectorization, and no reported production problems related to large-scale. Several production procedures can be applied to achieve high association efficiency between the bioactive and the carrier, depending on the physicochemical properties of both, as well as on the production procedure applied. The whole set of unique advantages such as enhanced drug loading capacity, prevention of drug expulsion, leads to more flexibility for modulation of drug release and makes Lipid-based nanocarriers (LNCs) versatile delivery system for various routes of administration. The route of administration has a significant impact on the therapeutic outcome of a drug. Thus, the non-invasive routes, which were of minor importance as parts of drug delivery in the past, have assumed added importance drugs, proteins, peptides and biopharmaceuticals drug delivery and these include nasal, buccal, vaginal and transdermal routes. The objective of this paper is to present the state of the art concerning the application of the lipid nanocarriers designated for non-invasive routes of administration. In this manner, this review presents an innovative technological platform to develop nanostructured delivery systems with great versatility of application in non-invasive routes of administration and targeting drug release.


2017 ◽  
Vol 23 (3) ◽  
pp. 467-480 ◽  
Author(s):  
Satyanarayan Pattnaik ◽  
Kamla Pathak

Background: Improvement of oral bioavailability through enhancement of dissolution for poorly soluble drugs has been a very promising approach. Recently, mesoporous silica based molecular sieves have demonstrated excellent properties to enhance the dissolution velocity of poorly water-soluble drugs. Description: Current research in this area is focused on investigating the factors influencing the drug release from these carriers, the kinetics of drug release and manufacturing approaches to scale-up production for commercial manufacture. Conclusion: This comprehensive review provides an overview of different methods adopted for synthesis of mesoporous materials, influence of processing factors on properties of these materials and drug loading methods. The drug release kinetics from mesoporous silica systems, the manufacturability and stability of these formulations are reviewed. Finally, the safety and biocompatibility issues related to these silica based materials are discussed.


2020 ◽  
pp. 1-9
Author(s):  
Yunhong Wang ◽  
Rong Hu ◽  
Yanlei Guo ◽  
Weihan Qin ◽  
Xiaomei Zhang ◽  
...  

OBJECTIVE: In this study we explore the method to prepare tanshinone self-microemulsifying sustained-release microcapsules using tanshinone self-microemulsion as the core material, and chitosan and alginate as capsule materials. METHODS: The optimal preparation technology of chitosan-alginate tanshinone self-microemulsifying sustained-release microcapsules was determined by using the orthogonal design experiment and single-factor analysis. The drug loading and entrapment rate were used as evaluation indexes to assess the quality of the drug, and the in vitro release rate was used to evaluate the drug release performance. RESULTS: The best technology of chitosan-alginate tanshinone self-microemulsifying sustained-release microcapsules is as follows: the concentration of alginate is 1.5%, the ratio of tanshinone self-microemulsion volume to alginate volume to chitosan mass is 1:1:0.5 (ml: ml: g), and the best concentration of calcium chloride is 2.0%. To prepare the microcapsules using this technology, the drug loading will be 0.046%, the entrapment rate will be 80.23%, and the 24-hour in vitro cumulative release rate will be 97.4%. CONCLUSION: The release of the microcapsules conforms to the Higuchi equation and the first-order drug release model and has a good sustained-release performance.


Sign in / Sign up

Export Citation Format

Share Document