Investigation on the Formulation Factors Influencing Drug Loading Capacity and Encapsulation Efficiency of Lisinopril Loaded Polyvinyl Alcohol Micro-particles

Abstract

Abstract:

Objective: To investigate the formulation factors influencing drug loading capacity and encapsulation efficiency （EE）of lisinopril-loaded polyvinyl alcohol（PVA）micro-particles（LIS-PVA-MP）. Methods: LIS-PVA-MP was prepared by spray-drying and the formulation factors influencing drug loading capacity and EE such as hydrolysis degree （HD）of PVA, molecular weight （Mw）of PVA, concentration of PVA and weight ratio of lisinopril to PVA in the feed solution were investigated by single factor experiments. Results: Differences were analyzed by one-way analysis of variance （ANOVA）. At the 0.05 level, the means are significantly different in the factors such as HD of PVA, concentration of PVA and weight ratio of lisinopril to PVA in the feed solution. However, at the 0.05 level, the means are not significantly different in the factor of Mw of PVA. Conclusion: All of the three factors, HD of PVA, concentration of PVA and weight ratio of lisinopril to PVA in the feed solution, have a significant influence on drug loading capacity and EE of LIS-PVA-MP.

Key words: lisinopril, micro-particles, drug loading capacity, encapsulation efficiency

CLC Number:

R972

WU Jun-Zhu, WANG Cheng-Jun, JIN Tuo. Investigation on the Formulation Factors Influencing Drug Loading Capacity and Encapsulation Efficiency of Lisinopril Loaded Polyvinyl Alcohol Micro-particles[J]. J4, 2010, 9(2): 6-10.

References

〔1〕WALD N J，LAWM R. A strategy to reduce cardiovascular
disease by more than 80%〔J〕. BMJ，2003，326（7404）：
1419-1424.
〔2〕Fahey T，Brindle P，Ebrahim S. The polypill and
cardiovascular disease-May be appropriate for secondary，
but perhaps not for primary prevention〔J〕.BMJ，2005，330
（7499）：1035-1036.
〔3〕Robinson JG， Maheshwari N. A“poly -portfolio”for

secondary prevention：A strategy to reduce subsequent
events by up to 97% over five years〔J〕. AM J CARDIOL，
2005，95（3）：373-378.
〔4〕Don Poldermans，Robert Glazes，Stefanos Kargiannis，et
al. Tolerability and blood pressure-lowering efficacy of the
combination of amlodipine plus calsartan compared with
lisinopril plus hydrochlorothiazide in adult patients with
stage 2 hypertension〔J〕. Clinical Therapeutics，2007，29
（2）：279-289.
〔5〕David S Wald，Malcolm Law，Sarah Mills，et al. A
16-week，randomized，double-blind，placebo-controlled，
crossover trial to quantify the combined effect of an
angiotensin-converting enzyme inhibitor and a 茁-blocker
on blood pressure reduction〔J〕.Clinical Therapeutics，
2008，30（11）：2030-2039.
〔6〕Vijay Kumar， Bhagwat Prasad， Saranjit Singh .
Pharmaceutical issues in the development of a polypill for
the treatment of cardiovascular diseases〔J〕. Drug Discovery
Today：Therapeutic Strategies，2008，5（1）：63-71.
〔7〕Arthur H Kibbe. Handbook of pharmaceutical excipients
（3rd Edition）〔M〕.London：Pharmaceutical Press，2000：
424-425.
〔8〕Yong-Hong Liao，Marc B. Brown，Stuart A Jones，et al.
The effects of polyvinyl alcohol on the in vitro stability and
delivery of spray-dried protein particles fromsurfactant-free
HFA 134a-based pressurised metered dose inhalers〔J〕.
International Journal of Pharmaceutics，2005，304（1-2）：
29-39.
〔9〕OZMEN L，LANGRISH T A G，GIPPS E M. Spray drying
pharmaceutical products for nasal delivery：The effects of
feed solution properties and operating conditions on particle
size and density〔C〕/Leonardi E，Madhusudana C V. Heat
and Mass Transfer Australasia Proceedings of the Sixth
Australasian： Heat and Mass Transfer Conference，
December 9 -12，1996，Sydney，Australia. New York：
Begell House，1998：427-434.
〔10〕The United States Pharmacopeial Convention. The United
States Pharmacopeia〔S〕. Rockville，USA：2005（USP28-
NF23）：1139-1140.